Chromatine/Épigénétique
Les inhibiteurs de la chromatine/épigénétique sont des composés qui modulent la structure et la fonction de la chromatine ou interfèrent avec les modifications épigénétiques, telles que la méthylation de l'ADN et la modification des histones. Ces inhibiteurs sont des outils essentiels pour étudier la régulation de l'expression génique et le rôle de l'épigénétique dans des maladies telles que le cancer, les troubles neurologiques et les anomalies du développement. En ciblant les processus épigénétiques, ces inhibiteurs peuvent modifier les schémas d'expression génique et offrir de nouvelles perspectives thérapeutiques. Chez CymitQuimica, nous offrons une large sélection d'inhibiteurs de la chromatine/épigénétique de haute qualité pour soutenir vos recherches en biologie moléculaire, génétique et épigénétique.
Sous-catégories appartenant à la catégorie "Chromatine/Épigénétique"
2400 produits trouvés pour "Chromatine/Épigénétique"
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SMARCA2-IN-6
CAS :<p>SMARCA2-IN-6 is a potent inhibitor of SMARCA2 (also known as BRM), exhibiting an IC50 of less than 5 nM against both SMARCA2 and SMARCA4. Additionally, this compound suppresses the expression of the KRT80 gene in H1299 cells with an IC50 of 26 nM and inhibits the proliferation of SKMEL5 cells carrying a BRG1 mutation with an IC50 value of 13 nM.</p>Formule :C10H8ClF2N5OSCouleur et forme :SolidMasse moléculaire :319.72HDAC6-IN-3
HDAC6-IN-3 (Compound 14) is an oral anti-prostate cancer agent, inhibiting HDACs and MAO-A, with IC50 of 0.02-1.54 μM.Formule :C19H27N3O3Couleur et forme :SolidMasse moléculaire :345.44MAT2A-IN-24
CAS :<p>MAT2A-IN-24 (Compound 9) is an inhibitor of methionine adenosyltransferase 2a (MAT2a), with an IC50 value of 20 nM for MAT2a inhibition and an antiproliferative IC50 value of 10 nM for HAP1MTAP–/– cells. MAT2A-IN-24 is applicable in the research of tumor diseases associated with MTAP deficiency.</p>Formule :C32H33Cl2N7O2Couleur et forme :SolidMasse moléculaire :618.556JTZ-951 HCl
CAS :JTZ-951 is a potent and orally active inhibitor of hypoxia inducible factor prolyl hydroxylase (PHD).Formule :C17H17ClN4O4Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :376.79HIF-2α-IN-5
CAS :<p>HIF-2α-IN-5 is a potent HIF-2α inhibitor with an IC 50 of < 50 nM [1].</p>Formule :C15H12F4O3S2Couleur et forme :SolidMasse moléculaire :380.38EN884
CAS :EN884 is a BRD4 degrader that functions through an SKP1 and proteasome-dependent degradation pathway. It is utilized in the synthesis of proteolysis-targeting chimeras (PROTAC).Formule :C14H18N2OMasse moléculaire :230.31HDAC8-IN-2
<p>HDAC8-IN-2 (5o) inhibits both smHDAC8 and hHDAC8 with IC50s of 0.27 μM, 0.32 μM, kills schistosome larvae, and lowers egg laying.</p>Formule :C21H16N2O5Couleur et forme :SolidMasse moléculaire :376.36CCW 28-3
CAS :CCW 28-3 is a novel potent covalent BRD4 degrader, degrading BRD4 in a proteasome- and RNF4-dependent manner without inhibiting RNF4 autoubiquitination activityFormule :C44H42Cl2N6O4SCouleur et forme :SolidMasse moléculaire :821.81EBET-590
CAS :EBET-590 is a BET inhibitor utilized in cancer research.Formule :C26H26N4O3Masse moléculaire :442.51AR/BET protein degrader-1
CAS :AR/BET protein degrader-1 (Compound 149) is a dual-targeting protein degrader of Androgen Receptor and BET (bromodomain and extra-terminal domain), suitable for cancer research.Formule :C43H44N6O5Masse moléculaire :724.85BSI-401
CAS :BSI-401 is an oral inhibitor of PARP-1. It can inhibit pancreatic cancer either when used alone or in synergy with Oxaliplatin.Formule :C9H4INO4Couleur et forme :SolidMasse moléculaire :317.037BRD4/NAMPT-IN-1
CAS :BRD4/NAMPT-IN-1 (Compound A2) exhibits strong inhibitory effects on NAMPT and BRD4, with IC50 values of 35 nM (NAMPT) and 58 nM (BRD4). This compound significantly suppresses the growth and migration of liver cancer cells while promoting apoptosis. Additionally, BRD4/NAMPT-IN-1 demonstrates potent anticancer activity in HCCLM3 xenograft mouse models without noticeable toxicity.Formule :C30H30ClN7O2SMasse moléculaire :588.12W4275
CAS :W4275 (Compound 42) is a selective NSD2 inhibitor with oral activity and an IC50 of 17 nM. It exhibits antiproliferative activity, with an IC50 of 230 nM against RS411 cells, and significantly inhibits tumor growth in an RS411 tumor xenograft model. Pharmacokinetic analysis in mice shows that W4275 has a favorable oral bioavailability (F is 27.34%). W4275 holds potential for use in cancer research.Formule :C25H36N6O3Couleur et forme :SolidMasse moléculaire :468.59MAT2A-IN-21
CAS :<p>MAT2A-IN-21 (compound 28) is a potent inhibitor of methionine adenosyltransferase 2A (MAT2A), with an IC50 of 49 nM. It selectively inhibits cancer cells with MTAP deficiency.</p>Formule :C26H20F2N4O2Couleur et forme :SolidMasse moléculaire :458.459Trichostatin A S-isomer
CAS :Trichostatin A S-isomer, a HDAC 1, 3, 4, 6, 10 inhibitor with IC50 ~20 nM, has wide-ranging epigenetic effects.Formule :C17H22N2O3Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :302.3715:0 PG sodium
CAS :15:0 PG sodium serves as an activator for the Protein Kinase C family and is an anionic phospholipid located in the membranes of mitochondria and microsomes. It plays a crucial role in the composition of pulmonary surfactants, especially within the membrane of the pulmonary lamellar bodies.Formule :C36H70NaO10PCouleur et forme :SolidMasse moléculaire :716.90TYK2 ligand 2
CAS :<p>TYK2ligand 2 is the TYK2 ligand of PROTACTYD-68. TYD-68 is a highly potent and selective CRBN-recruiting TYK2 PROTAC degrader with a DC50 value of 0.42 nM.</p>Formule :C24H20FN7O4Couleur et forme :SolidMasse moléculaire :489.458Octyl-α-hydroxyglutarate
CAS :<p>Octyl-α-hydroxyglutarate (octyl-2-HG) enhances histone methylation and boosts the viability of LMP1-negative nasopharyngeal carcinoma (NPC) cells.</p>Formule :C13H24O5Masse moléculaire :260.33Itareparib
CAS :Itareparib is a PARP inhibitor with demonstrated antitumor activity.Formule :C20H26FN3O2Couleur et forme :SolidMasse moléculaire :359.438LSD1-IN-22
<p>LSD1-IN-22: potent LSD1 inhibitor, K_i 98 nM, curbs cancer cell growth.</p>Formule :C9H8BrF2NCouleur et forme :SolidMasse moléculaire :248.07Pociredir
CAS :Pociredir (FTX-6058), a potent EED inhibitor (KD=0.163 nM), may help in SCD research.Formule :C22H18FN5O2Couleur et forme :SolidMasse moléculaire :403.41PRMT5-MTA-IN-3
CAS :<p>PRMT5-MTA-IN-3 (Compound P2A) is an orally active and selective inhibitor of protein arginine methyltransferase 5 (PRMT5). It inhibits the proliferation of MTAP-deficient colorectal cancer HCT-116 cell line with an IC50 value of 5 nM. PRMT5-MTA-IN-3 holds potential for research in cancers, particularly in MTAP-deficient tumors such as colorectal cancer, non-small cell lung cancer, and pancreatic cancer.</p>Formule :C19H17F3N6O3Couleur et forme :SolidMasse moléculaire :434.372CBP/p300-IN-18
CBP/p300-IN-18 (compound 8) is a potent inhibitor of EP300/CBP HAT, acting on HAT EP300 (IC50: 0.056 μM) and LK2 H3K27 (IC50: 0.46 μM).Formule :C25H27FN4O3Couleur et forme :SolidMasse moléculaire :450.51LSD1-IN-15
LSD1-IN-15 inhibits LSD1, MAO-A/B with IC50s: 0.149, 0.028, 0.327 μM; arrests LNCaP cancer cell growth, IC50 9.9 μM.Formule :C22H20N2OCouleur et forme :SolidMasse moléculaire :328.41Purinostat
CAS :Purinostat is a selective inhibitor of HDACI/IIb with potential anti-leukemic properties. Its mesylate form, Purinostat mesylate, is effective at inhibiting the survival of Ph+ leukemic cells and CD34+ leukemic cells derived from CML patients. Purinostat mesylate targets HDACI/IIb, impacting several crucial factors for leukemia stem cell (LSC) survival, such as c-Myc, β-Catenin, E2f, Ezh2, Alox5, and mTOR. Additionally, Purinostat mesylate enhances glutamate metabolism in LSCs by increasing GLS1.Formule :C23H26N10O3Couleur et forme :SolidMasse moléculaire :490.518HuR degrader 2
CAS :<p>HuRdegrader 2 (Compound 3) is a molecular glue that targets and degrades the RNA-binding protein Hu antigen R (HuR), achieving 30% degradation at 0.1 μM. It inhibits the proliferation of Colo-205 cancer cells with an IC50 of ≤200 nM. HuRdegrader 2 also shows high affinity for cereblon with an HTRF ratio < 0.02.</p>Formule :C20H15N3O3Masse moléculaire :345.35AMPK activator 16
CAS :AMPK activator16 (compound 6) functions as an AMP-activated protein kinase (AMPK) inhibitor. It interacts effectively with crucial AMPK residues, significantly activating the enzyme. In N2a cells, AMPK activator16 enhances the expression of phosphorylated AMPK (p-AMPK) and its downstream signaling proteins, such as phosphorylated ACC (Acetyl-CoA Carboxylase) and phosphorylated raptor (p-raptor).Formule :C23H20ClNO5SCouleur et forme :SolidMasse moléculaire :457.927LSD1-IN-39
CAS :<p>LSD1-IN-39 (Compound 14) is a reversible inhibitor of LSD1 with an IC50 of 0.18 μM, showing broad-spectrum antiproliferative activity against cancer cells, inhibiting HepG2 cell migration, and suppressing epithelial-mesenchymal transition. Additionally, LSD1-IN-39 exhibits antitumor activity in mouse models.</p>Formule :C25H30N2O7Couleur et forme :SolidMasse moléculaire :470.515DDO-3055
CAS :<p>DDO-3055 is an orally active PHD2 inhibitor utilized in studies related to anemia associated with chronic kidney disease.</p>Formule :C17H13ClN2O5Couleur et forme :SolidMasse moléculaire :360.749lirucitinib
CAS :<p>Lirucitinib is a JAK inhibitor known for its anti-inflammatory properties.</p>Formule :C16H25N5OSCouleur et forme :SolidMasse moléculaire :335.468LNK01004
CAS :<p>LNK01004 is a JAK inhibitor that exhibits potent inhibitory effects on JAK1 (IC50: 10 nM), JAK2 (IC50: ＜0.51 nM), and TYK2 (IC50: 1.0 nM). It can concurrently inhibit multiple cytokine-induced p-STAT signaling pathways and is applicable for research on diseases such as atopic dermatitis.</p>Formule :C26H31N7O2Couleur et forme :SolidMasse moléculaire :473.57AZ-3
CAS :AZ-3 is a potent and selective JAK1 inhibitor (IC50: 34 nM).Formule :C20H28FN7Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :385.48DS79932728
CAS :<p>DS79932728 is an orally active inhibitor of G9a and GLP, with IC50 values of 12.6 nM and 75.7 nM, respectively. It induces the production of γ-globin, thereby increasing fetal hemoglobin (HbF) levels. In cynomolgus monkey models, DS79932728 enhances the proportion of F-reticulocytes (F-rets) and shows good oral absorption characteristics.</p>Formule :C19H25N3OCouleur et forme :SolidMasse moléculaire :311.421PRMT5-IN-48
CAS :PRMT5-IN-48 (compound D3) is an orally active PRMT5 inhibitor with an IC50 of 20.7 nM, displaying antitumor activity. It effectively suppresses the growth of various cancer cells, induces apoptosis, and causes cell cycle arrest at the G0/G1 phase. PRMT5-IN-48 is applicable for research in non-Hodgkin's lymphoma (NHL).Formule :C30H37N5O3Couleur et forme :SolidMasse moléculaire :515.646Menin-MLL inhibitor 4
CAS :Menin-MLL inhibitor 4 has antitumor activity.Menin-MLL inhibitor 4 is an inhibitor of Menin- MLL (mixed-lineage leukemia protein) interaction .Formule :C32H38FN7O3Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :587.69HDAC11-IN-2
CAS :<p>HDAC11-IN-2 (compound B6) is a highly selective inhibitor of Histone Deacetylase 11 (HDAC11). It demonstrates IC50 values of 51.1 ×10^-3 μM for HDAC11 and 5 μM for HDAC8. HDAC11-IN-2 reduces de novo lipogenesis (DNL) and enhances fatty acid oxidation, which alleviates hepatic lipid accumulation and pathological symptoms in MASLD mice. By inhibiting HDAC11, HDAC11-IN-2 enhances the phosphorylation of AMPKα1 at the Thr172 site, thereby modulating de novo lipogenesis and fatty acid oxidation in the liver.</p>Formule :C25H35N3O3Couleur et forme :SolidMasse moléculaire :425.564PARP1-IN-29
CAS :<p>PARP1-IN-29 is an orally active PARP-1 inhibitor with an IC50 of 6.3 nM. When labeled with [18F], PARP1-IN-29 can be utilized for positron emission tomography (PET) imaging, specifically targeting PARP-1 in tumors. This compound is useful in oncology and imaging studies, particularly for detecting PARP-1 activity in cancer.</p>Formule :C18H16FN3O2Couleur et forme :SolidMasse moléculaire :325.34Milpecitinib
CAS :<p>Milpecitinib (Compound 21a) is a potent and selective Janus tyrosine kinase (JAK) inhibitor with anti-inflammatory properties. It shows promise for research in cancer and inflammatory diseases.</p>Formule :C20H20N4O2SCouleur et forme :SolidMasse moléculaire :380.463SGC6870N
CAS :<p>SGC6870N is inactive against PRMT6 and can be used as a negative control. It is the inactive enantiomer of SGC6870.</p>Formule :C23H21BrN2O2SMasse moléculaire :469.39SIRT-IN-6
CAS :<p>SIRT-IN-6 (Compound 14) is a pan-inhibitor of SIRT1/2/3 with an IC50 value of >50 μM. It shows potential as a research agent for studies involving metabolic disorders, inflammation, cancer, and neurodegenerative diseases.</p>Formule :C7H4ClN3OSCouleur et forme :SolidMasse moléculaire :213.644PHD2-IN-4
CAS :<p>PHD2-IN-4 (compound 1) is an inhibitor of PHD2, with an IC50 of 4 nM. It is utilized in research related to chronic kidney disease.</p>Formule :C21H19N5O3Couleur et forme :SolidMasse moléculaire :389.407HDAC-IN-87
CAS :<p>HDAC-IN-87 (Compound XII6) is a non-selective HDAC inhibitor with pIC50 values of 6.9 for HDAC4 and 5.8 for HDAC6. It exhibits fungicidal activity against P. sorghi and P. pachyrhizi. The acute oral LD50 in both male and female rats is greater than 500 mg/kg.</p>Formule :C13H7F5N4O2SCouleur et forme :SolidMasse moléculaire :378.277BET/Aurora kinase-IN-1
CAS :<p>BET/Aurora kinase-IN-1 (Compound 38) is a dual inhibitor of BET and Aurora kinases. It exhibits antiproliferative activity against various tumor cell lines and demonstrates significant antitumor efficacy in xenograft models of renal cell carcinoma and colon cancer, with tumor growth inhibition (TGI) rates of 45.99% and 53.06%, respectively.</p>Formule :C25H30FN7OCouleur et forme :SolidMasse moléculaire :463.55FT001
CAS :FT001: Oral BET Bromodomain inhibitor, IC50=0.46μM, suppresses MYC, anti-cancer, effective in vitro/vivo.Formule :C25H29N3O4SDegré de pureté :99.9%Couleur et forme :SolidMasse moléculaire :467.58(rac)-Talazoparib
CAS :<p>(rac)-Talazoparib ((rac)-BMN-673) (Compound 47) is an orally active inhibitor of PARP1/2, with Ki values of 1.2 nM and 0.87 nM, respectively. It inhibits cellular PARylation at an EC50 of 2.51 nM. This compound leads to the accumulation of DNA damage and suppresses the proliferation of BRCA1/2-mutated MX-1 and Capan-1 cells, with IC50 values of 0.3 nM and 5 nM, respectively. Additionally, (rac)-Talazoparib exhibits antitumor activity in mouse models.</p>Formule :C19H14F2N6OCouleur et forme :SolidMasse moléculaire :380.351Aurora B inhibitor 1
CAS :Aurora B inhibitor 1 is an Aurora B (Aurora-1) inhibitor (Ki <0.010 uM) with potential anticancer activity for cancer research.Formule :C25H26ClF2N7O2Degré de pureté :98.37%Couleur et forme :SolidMasse moléculaire :529.97BRD4-IN-7
CAS :BRD4-IN-7, also known as compound 120, acts as a BRD4 inhibitor.Formule :C29H24F2N4O3Couleur et forme :SolidMasse moléculaire :514.52BBC0403
CAS :<p>BBC0403 is a BRD2 inhibitor, inhibiting BRD2 and BRD2, and suppresses NF-κB and MAPK signaling pathways.</p>Formule :C21H22N2O5Degré de pureté :98.15%Couleur et forme :SolidMasse moléculaire :382.41PRMT5-IN-50
CAS :<p>PRMT5-IN-50 is an orally active selective inhibitor of PRMT5, demonstrating good metabolic stability and low clearance in human liver microsomes. It inhibits SDMA/HCT116-MTAPdel and SDMA/HCT116-MTAPwt with IC50 values for symmetric arginine methylation inhibition at 1.0 and 536 nM, respectively, and antiproliferative IC50 values at 19 and 1620 nM, respectively. Additionally, PRMT5-IN-50 suppresses tumor growth in mice.</p>Formule :C26H23F3N6OCouleur et forme :SolidMasse moléculaire :492.496BRD4 Inhibitor-33
CAS :<p>BRD4 Inhibitor-33 (example 13), a potent inhibitor of BRD4, is applicable in research related to both acute and chronic kidney diseases [1].</p>Formule :C24H20N4O2Couleur et forme :SolidMasse moléculaire :396.44PRMT5-IN-49
CAS :PRMT5-IN-49 (Compound 4b16) is an inhibitor of PRMT5.Formule :C19H22N2O2Couleur et forme :SolidMasse moléculaire :310.39NSD2-PWWP1-IN-2
CAS :NSD2-PWWP1-IN-2 (compound 33) is a potent NSD2-PWWP1 inhibitor, exhibiting an IC50 value of 1.49 µM, indicating its potential utility in cancer research.Formule :C29H30N4Couleur et forme :SolidMasse moléculaire :434.575NVS-BPTF-1
CAS :NVS-BPTF-1 is a specific inhibitor of bromodomain and PHD finger containing transcription factor (BPTF), exhibiting a dissociation constant (K_D) of 71 nM [1].Formule :C26H28FN7O3SCouleur et forme :SolidMasse moléculaire :537.61SRI-43265
CAS :<p>SRI-43265 (compound 40) inhibits the dimerization of human antigen R protein (HuR), which is involved in cancer and inflammation pathogenesis [1].</p>Formule :C19H20N6OCouleur et forme :SolidMasse moléculaire :348.4HYDAMTIQ
CAS :HYDAMTIQ, a PARP-1/2 inhibitor (IC 50 : 29-38 nM), exhibits a range of pharmacological effects including anticancer, anti-inflammatory, and ischemic protective properties. It effectively reduces pulmonary PARP activity and alleviates symptoms such as allergen-induced cough and dyspnea while also diminishing bronchial hyperresponsiveness to methacholine. Moreover, HYDAMTIQ shows potent tumor suppressor activity in various cancers such as ovarian, breast, prostate, pancreatic, and glioblastoma multiforme. Demonstrating in vivo efficacy, HYDAMTIQ has been tested in animal models for conditions like cerebral ischemia, asthma, and cancer [1].Formule :C14H14N2O2SCouleur et forme :SolidMasse moléculaire :274.34Tyk2-IN-20
CAS :Tyk2-IN-20 (Example 289) is an effective inhibitor of Tyk2 with an IC50 value below 5 nM. Additionally, it inhibits JAK1, JAK2, and JAK3 with IC50 values under 100 nM. This compound is utilized for the research of inflammatory diseases.Formule :C24H25N7O2Couleur et forme :SolidMasse moléculaire :443.50PRMT5-IN-37
CAS :PRMT5-IN-37 (compound 29), an orally active inhibitor of PRMT5, is utilized for cancer research.Formule :C21H15F4N5O2Couleur et forme :SolidMasse moléculaire :445.37STR-V-53
CAS :<p>STR-V-53, an HDAC inhibitor (IC50 in nM), increases histone acetylation in tumor cells by inhibiting these enzymes, thereby regulating gene expression. STR-V-53 inhibits tumor growth and induces apoptosis [1].</p>Formule :C21H30N4O8Couleur et forme :SolidMasse moléculaire :466.48HDAC3-IN-3
CAS :HDAC3-IN-3 (compound 31), a potent inhibitor of HDAC3, holds potential for cancer research [1].Formule :C26H22N4O2Couleur et forme :SolidMasse moléculaire :422.48GDC-9918
CAS :<p>GDC-9918 (compound GDC-9918) is an inhibitor of Janus kinases.</p>Formule :C20H18F2N6O5SCouleur et forme :SolidMasse moléculaire :492.46BRD4 Inhibitor-32
CAS :BRD4 Inhibitor-32 (example 15), a BRD4 inhibitor, is applicable in research pertaining to both acute and chronic kidney disease [1].Formule :C26H25N3O3Couleur et forme :SolidMasse moléculaire :427.5NSD2-PWWP1-IN-1
CAS :<p>NSD2-PWWP1-IN-1 (compound 31) is a potent inhibitor of NSD2-PWWP1 with an IC50 value of 0.64 µM, demonstrating potential applications in cancer research.</p>Formule :C28H30N4Couleur et forme :SolidMasse moléculaire :422.565RK-0080552
CAS :RK-0080552 (RK-552) is an inhibitor of the NSD2 histone methyltransferase. It demonstrates significant cytotoxicity against multiple myeloma (MM) cells harboring the t(4;14) translocation. This compound suppresses the IRF4 gene and decreases the dimethylation of histone H3 at lysine 36. RK-0080552 holds promise for research in hematologic malignancies.Formule :C12H6N6O2Couleur et forme :SolidMasse moléculaire :266.215JPHM-2-167
CAS :<p>PHM-2-167 (Compound 11) is a selective inhibitor of the prolyl hydroxylase domain enzyme (PHD). It inhibits PHD2 and PHD3 with IC50 values of 0.253 μM and 3.95 μM, respectively. PHM-2-167 is applicable for research in chronic kidney disease.</p>Formule :C30H28N6O2Couleur et forme :SolidMasse moléculaire :504.582GSK852
GSK852 is a potent, second bromodomain (BD2)-selective, bromo and extra-terminal domain (BET) inhibitor with pIC50 of 7.9.Formule :C24H26N2O4Couleur et forme :SolidMasse moléculaire :406.47SCR-7952
CAS :<p>SCR-7952, a MAT2A inhibitor, is utilized in cancer research.</p>Formule :C19H15ClN4OCouleur et forme :SolidMasse moléculaire :350.80Pim-1 kinase inhibitor 3
CAS :<p>Pim-1 kinase inhibitor 3 (Compound H5) is a potent inhibitor of Pim-1 kinase, demonstrating an inhibitory concentration (IC50) of 35.13 nM [1].</p>Formule :C20H25N3O2Couleur et forme :SolidMasse moléculaire :339.43LSD1/HDAC-IN-1
CAS :<p>LSD1/HDAC-IN-1 (compound 2) serves as an effective inhibitor of both HDAC and LSD1, demonstrating IC50 values of 0.125 nM, 0.373 nM, 0.0118 nM, 0.103 nM, and 0.571 μM for HDAC1, HDAC2, HDAC6, HDAC8, and LSD1 respectively. This compound plays a crucial role in cancer research.</p>Formule :C18H18N2O4SCouleur et forme :SolidMasse moléculaire :358.41BRD4 Inhibitor-17
BRD4 Inhibitor-17: Potent with 0.33 μM IC50; modulates gene expression, may counter arsenic toxicity.Formule :C16H16FN3O3SCouleur et forme :SolidMasse moléculaire :349.38O6BTG-C8-αGlu
CAS :<p>O6BTG-C8-αGlu is an O6-methylguanine-DNA methyltransferase (MGMT) inhibitor with an IC50 of 0.45 μM. At a concentration of 0.1 μM, it fully inhibits MGMT in HeLaS3 cells and demonstrates no cytotoxicity even at prolonged high doses (up to 20 μM). This compound is suitable for research on MGMT-related cancers.</p>Formule :C24H34BrN5O7SCouleur et forme :SolidMasse moléculaire :616.525FNDR-20123
FNDR-20123: First safe, effective anti-malarial HDAC inhibitor for Plasmodium (IC50: 31 nM) & human HDACs, with nanomolar potency across several subtypes.Formule :C21H24ClN5O2Couleur et forme :SolidMasse moléculaire :413.9Cenacitinib
CAS :Cenacitinib is an effective inhibitor of Janus kinase (Janus kinase) and possesses anti-inflammatory activity.Formule :C19H19F2N7O3Couleur et forme :SolidMasse moléculaire :431.40JAK3-IN-11
CAS :JAK3-IN-11: potent oral JAK3 inhibitor (IC50=1.7 nM), noncytotoxic, >588-fold selectivity, blocks T-cell growth; useful in autoimmune research.Formule :C23H23N5O2Couleur et forme :SolidMasse moléculaire :401.46Equisetin
CAS :Equisetin: a QSI from Fusarium equiseti, curbs P. aeruginosa virulence, fights Gram-positive bacteria & HIV-1 integrase; not antibacterial to Gram-negative.Formule :C22H31NO4Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :373.49PROTAC BRD4 Degrader-25
CAS :PROTAC BRD4 Degrader-25 (Compound 1-f), a targeted BRD4 degrader, is utilized in the study of cancer and additional diseases related to bromodomains [1].Formule :C34H30FN9O2SCouleur et forme :SolidMasse moléculaire :647.72YLIU-4-105-1
CAS :YLIU-4-105-1 is a type II JAK2 inhibitor. Demonstrating in vivo pharmacological activity, YLIU-4-105-1 reduces splenic weight, decreases blood reticulocyte counts in a dose-dependent manner, and inhibits pSTAT5.Formule :C32H34F3N7O2Couleur et forme :SolidMasse moléculaire :605.65P300 bromodomain-IN-1
P300 bromodomain-IN-1 blocks c-Myc, induces G1/G0 arrest, apoptosis. Potent EP300 inhibitor (IC50: 49 nM).Formule :C29H31ClN4O4Couleur et forme :SolidMasse moléculaire :535.03PFI-6-COOH
CAS :PFI-6-COOH (Compound 18) is a ligand for the eleven-nineteen leukemia (ENL) protein, and is utilized in the synthesis of the ENL PROTAC degrader MS41.Formule :C23H21N3O6Couleur et forme :SolidMasse moléculaire :435.43Aurora inhibitor 1
CAS :<p>Aurora inhibitor 1 is a potent Aurora inhibitor (IC50: ≤ 4 nM and ≤13 nM for Aurora A and Aurora B kinase).</p>Formule :C23H25N9SDegré de pureté :98%Couleur et forme :SolidMasse moléculaire :459.57HLCL-61
CAS :HLCL-61 is a premier small-molecule inhibitor of protein arginine methyltransferase 5 (PRMT5).Formule :C23H24N2OCouleur et forme :SolidMasse moléculaire :344.45KAT6A-IN-1
CAS :KAT6A-IN-1 (compound 5) is an inhibitor of KAT6A.Formule :C23H27N5O5SCouleur et forme :SolidMasse moléculaire :485.56KAT6A-IN-2
CAS :KAT6A-IN-2 (compound 7) is an inhibitor of KAT6A.Formule :C23H29N5O5SCouleur et forme :SolidMasse moléculaire :487.57MTL-CEBPA
MTL-CEPBA is a small activating RNA that targets C/EBPα upregulation and exhibits anti-inflammatory and anti-cancer effects.Couleur et forme :SolidAurora A inhibitor 1
CAS :Aurora A inhibitor 1: potent, selective, targets cancer-linked Aurora A overexpression, potential for cancer research. (WO2021147974A1, 49)Formule :C25H28ClF2N5O2Couleur et forme :SolidMasse moléculaire :503.97Balomenib
CAS :Balomenib is an inhibitor of the menin-MLL interaction, effectively blocking the men1-MLL4-43 interaction with an IC50 of less than 0.075 μM. It inhibits cell growth in MV4-11 (CC50 < 0.1 μM), MOLM-13 (CC50 0.1~0.5 μM), and HEK293 (CC50 < 2 μM) cells. Balomenib also exhibits antitumor activity.Formule :C33H34F3N7O2Couleur et forme :SolidMasse moléculaire :617.664PROTAC BRD4 ligand-4
CAS :PROTACBRD4 ligand-4 is a BRD4 ligand used in the synthesis of [PROTACBRD4 Degrader-37].Formule :C17H15NO4Couleur et forme :SolidMasse moléculaire :297.31JAK1/TYK2-IN-3
JAK1/TYK2-IN-3, orally active, selectively inhibits TYK2 (IC50: 6 nM), JAK1 (37 nM), JAK2 (140 nM), JAK3 (362 nM), and has anti-inflammatory effects.Couleur et forme :Solid6K465
CAS :6K465 is a potent Aurora A kinase inhibitor that reduces c-MYC and N-MYC oncoproteins, showing antiproliferative effects in SCLC and breast cancer cell lines.Formule :C26H33ClFN9ODegré de pureté :99.78%Couleur et forme :SolidMasse moléculaire :542.05Menin-MLL inhibitor 26
CAS :Menin-MLL inhibitor 26: Active reference, inhibits cell growth, used in leukemia research.Formule :C27H29F3N6O3SCouleur et forme :SolidMasse moléculaire :574.62MAT2A-IN-17
CAS :<p>MAT2A-IN-17 is a potent inhibitor of MAT2A, with an IC50 of less than 100 nM. MAT2A-IN-17 is applicable in cancer research.</p>Formule :C23H18F3N7OCouleur et forme :SolidMasse moléculaire :465.431WDR5-IN-5
CAS :WDR5-IN-5: Selective oral inhibitor for WDR5's WIN site with high affinity (Ki<0.02 nM) and anti-cancer properties. Good pharmacokinetics.Formule :C29H29F3N6OCouleur et forme :SolidMasse moléculaire :534.58PKCiota-IN-1
CAS :PKCiota-IN-1: Strong PKC-ι inhibitor (IC50=2.7 nM); also blocks PKC-α/ε (IC50s=45/450 nM).Formule :C25H22FN5OCouleur et forme :SolidMasse moléculaire :427.47Galegine hemisulfate
CAS :Galegine hemisulfate, a guanidine derivative, aids in weight reduction in mice. It activates AMPK in 3T3-L1 adipocytes, L6 myotubes, H4IIE rat hepatoma cells, and HEK293 human renal cell lines. Galegine hemisulfate also exhibits antibacterial activity, with a minimum inhibitory concentration of 4 mg/L against Staphylococcus aureus strains.Formule :C6H15N3O4SCouleur et forme :SolidMasse moléculaire :225.27PRMT5-IN-1 hydrochloride
PRMT5 IN-1 hydrochloride is a potent PRMT5 inhibitor (IC50: 11 nM), forms covalent adduct with C449, and converts to an aldehyde in vivo.Formule :C19H20Cl2N4O5Couleur et forme :SolidMasse moléculaire :455.29CARM1-IN-3 dihydrochloride
CARM1-IN-3 dihydrochloride (17b) is a potent CARM1 inhibitor (IC50: 0.07 μM) with selectivity over CARM3 (IC50 >25 μM).Formule :C24H34Cl2N4O2Couleur et forme :SolidMasse moléculaire :481.46BRD4 D1-IN-2
<p>BRD4 D1-IN-2 (compound 26), a BRD4 D1 inhibitor, IC50 <0.092 μM, 15 nM affinity, >500x selectivity over BRD2 D1/BRD4 D2.</p>Formule :C33H39F3N6OCouleur et forme :SolidMasse moléculaire :592.7PRMT5-IN-1
CAS :<p>PRMT5-IN-1 is a covalent inhibitor of protein arginine methyltransferase 5 (PRMT5)(IC50 of 11 nM for PRMT5/MEP50).</p>Formule :C19H19ClN4O5Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :418.83NI-Pano
NI-Pano (CH-03) is a novel hypoxia-activated KDAC inhibitor capable of O2-dependent release of the compound panobinostat.Formule :C26H28N6O4Couleur et forme :SolidMasse moléculaire :488.54JAK2 JH2 binder-1
CAS :JAK2 JH2 binder-1: potent, selective, Ki=37.1 nM, potential for studying myeloproliferative neoplasms.Formule :C29H25N7O6SCouleur et forme :SolidMasse moléculaire :599.62GDC-0339
CAS :GDC-0339: oral Pim kinase inhibitor for multiple myeloma (Kis: Pim1 - 0.03 nM, Pim2 - 0.1 nM, Pim3 - 0.02 nM), well-tolerated.Formule :C20H22F3N7OSCouleur et forme :SolidMasse moléculaire :465.5LSD1-IN-16
<p>LSD1-IN-16 (4b) inhibits LSD1, MAO-A/B; IC50: 0.015-0.366 μM. Halts prostate cancer cell growth; IC50: 15.2 μM.</p>Formule :C20H18N2OSCouleur et forme :SolidMasse moléculaire :334.43BRD-7880
CAS :BRD-7880 is a potent and highly specific inhibitor of aurora kinases B and C.Formule :C32H38N4O7Couleur et forme :SolidMasse moléculaire :590.67LSD1-IN-35
CAS :<p>LSD1-IN-35 (Compound Z-1) is a selective inhibitor of LSD1, exhibiting an IC50 of 108 nM. This compound inhibits the demethylation of H3K4me1/2 and acts as an immunomodulator. Additionally, LSD1-IN-35 enhances the responsiveness of gastric cancer cells to T-cell killing by reducing PD-L1 expression, thereby weakening the PD-1/PD-L1 interaction.</p>Formule :C25H26N4O2SCouleur et forme :SolidMasse moléculaire :446.57LSD1-IN-17
<p>LSD1-IN-17, a potent LSD1/CoREST/MAO inhibitor, IC50: 0.005/0.028/0.820 μM; hinders LNCaP prostate cancer cell growth, IC50: 17.2 μM.</p>Formule :C20H18N2OSCouleur et forme :SolidMasse moléculaire :334.43AZ13824374
AZ13824374: potent, selective ATAD2 inhibitor; anti-proliferative in breast cancer; pIC50: FRET 8.2, NanoBRET 6.2.Formule :C30H39FN8O2Couleur et forme :SolidMasse moléculaire :562.68LSD1/2-IN-3
LSD1/2-IN-3 selectively inhibits LSD1 (Ki 11 nM) over LSD2 (Ki 7 μM), and hinders tumor stem cell proliferation.Formule :C9H8BrF2NCouleur et forme :SolidMasse moléculaire :248.07AZ0108
CAS :AZ0108, an oral PARP1,2,6 inhibitor, selectively blocks centrosome clustering, is viable for in vivo studies, and doesn't inhibit PARP3/TNKS1.Formule :C24H20F4N6O2Couleur et forme :SolidMasse moléculaire :500.45HDAC/HSP90-IN-4
HDAC/HSP90-IN-4 inhibits HDAC (20 IC50=194nM, 26 IC50=360nM) & HSP90α (20 IC50=153nM, 26 IC50=77nM), affects cancer cell survival and invasion.Formule :C20H23N3O6Couleur et forme :SolidMasse moléculaire :401.15869RK-582
CAS :RK-582: oral spiroindolinone tankyrase inhibitor, halts colon cancer growth in COLO-320DM mouse model.Formule :C27H35FN6O3Couleur et forme :SolidMasse moléculaire :510.6PARP10/15-IN-1
PARP10/15-IN-1 (compound 8l) is a dual PARP10 and PARP15 inhibitor with IC50s of 160 nM and 370 nM, respectively. It can be used in cancer research[1].Formule :C13H10N2O3SCouleur et forme :SolidMasse moléculaire :274.3Ad-JQ1
CAS :Ad-JQ1 (Compound 16) is a Target Protein Ligand-Linker Conjugate incorporating a BRD4 ligand and a PROTAC linker capable of recruiting E3 ligase. It is utilized in the synthesis of PROTACβ-NF-JQ1.Formule :C37H47ClN6O4SCouleur et forme :SolidMasse moléculaire :707.33WIZ degrader 8
CAS :WIZ degrader 8 (compound 10) is a potent and selective molecular glue degrader of the transcription factor WIZ, effectively inducing HbF expression. It promotes WIZ degradation and HbF induction, suggesting its potential use as an inhibitor for sickle cell disease.Formule :C21H27N3O4Couleur et forme :SolidMasse moléculaire :385.457MMSET-IN-1
CAS :MMSET-IN-1 is an inhibitor of multiple myeloma SET domain (MMSET, aka NSD2/WHSC1) .Formule :C18H29N7O5Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :423.47HDAC-IN-33
HDAC-IN-33 inhibits HDAC1/2/6 (IC50: 24/46/47 nM), exhibits potent antitumor activity in vitro and in vivo, and activates antitumor immunity.Formule :C21H25N3O3Couleur et forme :SolidMasse moléculaire :367.44HDAC2-IN-1
HDAC2-IN-1 is an oral HDAC2 inhibitor (IC50: 0.5 μM), crosses the blood-brain barrier, and inhibits HDAC1 and HDAC8.Formule :C22H23ClN4OSCouleur et forme :SolidMasse moléculaire :426.96BRD4-BD1/2-IN-2
CAS :BRD4-BD1/2-IN-2 inhibits BRD4 BD1/BD2 with IC50 <300 nM/<0.5 nM (WO2021233371A1).Formule :C30H33N5O4Couleur et forme :SolidMasse moléculaire :527.61DS17701585
DS17701585: Oral EP300/CBP inhibitor; potent on CBP, EP300, H3K27, & SOX2; useful for cancer research.Formule :C24H26N4O5SCouleur et forme :SolidMasse moléculaire :482.55BET-IN-8
BET-IN-8 (Compound 27) is a potent inhibitor of BET (Ki: 0.83 μM, Kd: 0.571 μM), which ameliorates LPS-induced sepsis in vivo.BET-IN-8 has shown potential inFormule :C22H21N3O4SCouleur et forme :SolidMasse moléculaire :423.48B026
CAS :<p>B026: Oral p300/CBP HAT inhibitor, IC50: p300 1.8 nM, CBP 9.5 nM; targets AR+ prostate cancer cells.</p>Formule :C27H23F4N5O4Couleur et forme :SolidMasse moléculaire :557.5Tyk2-IN-15
CAS :<p>Tyk2-IN-15 (Compound 97) is a selective inhibitor of tyrosine kinase 2 (Tyk2) with an IC50 value ≤ 10 nM for Tyk2-JH2. It is utilized in the research of inflammatory and autoimmune diseases [1].</p>Formule :C21H25F2N7OCouleur et forme :SolidMasse moléculaire :429.47iBRD4-BD1 diTFA
CAS :iBRD4-BD1 diTFA is a selective BRD4 bromodomain inhibitor with an IC50 value of 12 nM. It can be used for research in inflammation and oncology [1].Formule :C33H32F9N5O5Couleur et forme :SolidMasse moléculaire :749.62SMARCA2/4-ligand-5
CAS :<p>SMARCA2/4-ligand-5 is the target protein ligand of PROTAC SMARCA2/4 degrader-37 (Example 4). PROTAC SMARCA2/4 degrader-37 (Example 4) is a PROTAC degrader of SMARCA2/4, with an IC50 value of ≤0.1 μM.</p>Formule :C20H13ClN4O3Couleur et forme :SolidMasse moléculaire :392.795Enzomenib
CAS :<p>Enzomenib (DSP5336), a menin protein inhibitor encoded by the multiple endocrine neoplasia (MEN) gene, blocks the interaction between menin protein and mixed lineage leukemia (MLL) fusion proteins. This compound is utilized in researching hematological malignancies.</p>Formule :C33H43FN6O3Couleur et forme :SolidMasse moléculaire :590.73(Rac)-RG108
CAS :<p>(Rac)-RG108 (NSC401077) is an inhibitor of DNMT1, effectively blocking DNA methyltransferases.</p>Formule :C19H14N2O4Couleur et forme :SolidMasse moléculaire :334.326GSK8814
CAS :GSK8814 is a selective and ATAD2/2B bromodomain chemical probe and inhibitor (binding constant pKd=8.1 and a pKi=8.9 in BROMOscan).Formule :C28H35F2N5O3Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :527.61JAK1/TYK2-IN-4
CAS :JAK1/TYK2-IN-4 serves as a dual inhibitor targeting both JAK and TYK2, displaying IC50 values of 39 nM and 21 nM, respectively. It is also orally bioavailable [1].Formule :C17H23N7OCouleur et forme :SolidMasse moléculaire :341.41BRD9 Degrader-2
CAS :BRD9 Degrader-2 (Compound B11), a potent BRD9 degrader (DC50≤1.25nM; Dmax≥75%), is applicable in cancer research.Formule :C40H43F3N6O4SCouleur et forme :SolidMasse moléculaire :760.87LSD1-IN-19
LSD1-IN-19 is a potent, selective LSD1 inhibitor with Ki of 0.108 μM and 72h IC50 values of 0.17-0.40 μM.Formule :C33H42N6O2Couleur et forme :SolidMasse moléculaire :554.73KDOAM-25 trihydrochloride
KDOAM-25 trihydrochloride selectively inhibits KDM5 enzymes, boosts H3K4 methylation, and suppresses MM1S cell growth.Formule :C15H28Cl3N5O2Couleur et forme :SolidMasse moléculaire :416.77Protein kinase inhibitor 7
CAS :Protein kinase inhibitor 7 functions as an inhibitor of protein kinase A (PKA) and protein kinase C (PKC). It impacts the autocrine motility factor (AMF) signaling pathway without affecting cell motility.Formule :C12H15N3O2SMasse moléculaire :265.33BET-IN-1
BET-IN-1 is a potent inhibitor of BET, exhibiting good brain permeability and a reasonable metabolic stability.Formule :C23H24ClFN4O3SCouleur et forme :SolidMasse moléculaire :490.98TDI-015051
CAS :TDI-015051 is an orally active inhibitor of SARS-CoV-2 non-structural protein 14 (SARS-CoV-2 NSP14) with an IC50 of ≤0.15 nM. It effectively inhibits SARS-CoV-2 NSP14 in Huh-7.5 cells (EC50=11.4 nM) and A549 cells expressing ACE2-TMPRSS2 (EC50=64.7 nM). Additionally, TDI-015051 suppresses other coronaviruses such as α-hCoV-NL63, α-hCoV-229E, and β-hCoV-MERS with IC50 values of 1.7, 2.6, and 3.6 nM, respectively. This compound inhibits viral RNA methylation and replication by binding to a stable SAH-cap pocket and demonstrates anti-infection activity in mouse models.Formule :C22H22FN5O4SCouleur et forme :SolidMasse moléculaire :471.505PF-06726304 acetate
CAS :<p>PF-06726304 acetate is a selective inhibitor of EZH2, with robust antitumor growth activity.</p>Formule :C24H25Cl2N3O5Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :506.38PARP7-IN-12
CAS :PARP7-IN-12, a potent inhibitor targeting PARP7, exhibits an IC50 of 7.836 nM. This compound is applicable in cancer research.Formule :C23H27ClF3N5O5Couleur et forme :SolidMasse moléculaire :545.94EZH2-IN-12
EZH2-IN-12 (Compound 5) is a potent inhibitor of EZH2, which has potential for studies of CNS malignancies.Formule :C23H23Cl2N3O3Couleur et forme :SolidMasse moléculaire :460.35Sapintoxin D
CAS :Sapintoxin D is a fluorescent phorbol ester and selective activator of protein kinase C.Formule :C30H37NO8Couleur et forme :SolidMasse moléculaire :539.62CRV431
CAS :CRV431 is a novel Pan-Cyclophilin Inhibitor, potently inhibiting all cyclophilin isoforms tested - A, B, D, and G (IC50 values ranged from 1-7 nM).Formule :C67H122N12O13Couleur et forme :SolidMasse moléculaire :1303.765-AIQ hydrochloride
CAS :<p>5-AIQ hydrochloride is a water-soluble PARP-1 inhibitor and serves as a vital functional group in various medications. It mitigates tissue damage associated with hepatic ischemia-reperfusion, making it valuable for research into conditions related to liver ischemia-reperfusion.</p>Formule :C9H9ClN2OCouleur et forme :SolidMasse moléculaire :196.634GSK3368715
CAS :GSK3368715 is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50sFormule :C20H38N4O2Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :366.54MAT2A-IN-19
CAS :<p>MAT2A-IN-19 (Compound I-3) is an inhibitor of methionine adenosyltransferase 2A (MAT2A), with an IC50 of 32.93 nM.</p>Formule :C23H15F5N6O3Couleur et forme :SolidMasse moléculaire :518.396SE-7552
CAS :<p>SE-7552, a derivative of 2-(difluoromethyl)-1,3,4-oxadiazole (DFMO), serves as an orally active, highly selective non-hydroxamate HDAC6 inhibitor, boasting an IC50 of 33 nM. It exhibits over 850-fold selectivity against all other known HDAC isozymes. Demonstrating efficacy in vivo, SE-7552 effectively inhibits the growth of multiple myeloma. Additionally, it functions as an anti-obesity agent in diet-induced obese mice [1] [2].</p>Formule :C15H12F3N5OCouleur et forme :SolidMasse moléculaire :335.28Glycyl H-1152 hydrochloride
CAS :<p>Glycyl-H-1152 is a potent ROCK-II inhibitor (IC50=11.8 nM) with high selectivity over CaMKII, PKG, Aurora A, PKA, and PKC. Better than Y-27632 and HA-1077.</p>Formule :C18H26Cl2N4O3SCouleur et forme :SolidMasse moléculaire :449.39M-525
CAS :M-525, a potent first-in-class menin-MLL inhibitor, binds at 3 nM IC50 and curbs MLL leukemia cell growth & gene expression.Formule :C39H51FN6O5SDegré de pureté :98%Couleur et forme :SolidMasse moléculaire :734.92G-631
CAS :<p>G-631 acts as a selective tankyrase inhibitor, effectively hindering tankyrase auto-PARsylation (poly ADP ribosylation) at an IC 50 of 7 nM and suppressing the Wnt signaling pathway. This compound also demonstrates favorable pharmacokinetic properties in mice.</p>Formule :C19H22F2N6O3Couleur et forme :SolidMasse moléculaire :420.41Aurora/LIM kinase-IN-1
Aurora/LIM kinase-IN-1 (Compound F114) is a dual inhibitor targeting aurora and lim kinases, potentially useful in GBM cancer treatment efforts.Formule :C16H20N6OCouleur et forme :SolidMasse moléculaire :312.37AFM-30a hydrochloride
AFM-30a hydrochloride: selective PAD2 inhibitor, EC50 9.5 μM; blocks H3 guanylation, EC50 0.4 μM; used for cancer and autoimmune research.Formule :C24H28ClFN6O3Couleur et forme :SolidMasse moléculaire :502.97PAD4-IN-5
CAS :<p>PAD4-IN-5 (Example 18) is a PAD4 inhibitor with an IC50 of ≤10 nM at 50 µM Ca2+ and 101-500 nM at 1 mM Ca2+ against human PAD4 (hPAD4). This compound is applicable in the study of autoimmune diseases such as rheumatoid arthritis (RA).</p>Formule :C34H41N7O3Couleur et forme :SolidMasse moléculaire :595.734Streptonigrin (racemate)
CAS :Streptonigrin: aminoquinone antibiotic; antitumor, antibacterial; blocks β-Catenin/Tcf, cytotoxic; alters hamster chromosomes; (-)-isomer, CAS#3930-19-6.Formule :C25H22N4O8Couleur et forme :SolidMasse moléculaire :506.46MAT2A-IN-20
CAS :<p>MAT2A-IN-20 (Compound A49) is an inhibitor of methionine adenosyltransferase 2A (MAT2A) with an IC50 of ≤50 nM. It also inhibits human UGT1A1 with an IC50 of 28.45 μM. Additionally, MAT2A-IN-20 exhibits antitumor activity in mouse models.</p>Formule :C26H24F2N6O4Couleur et forme :SolidMasse moléculaire :522.503JAK-IN-23
"JAK-IN-23: oral dual JAK/STAT & NF-κB inhibitor; JAK1 (IC50: 8.9 nM), JAK2 (15 nM), JAK3 (46.2 nM); for IBD research."Formule :C23H22Cl2N4OCouleur et forme :SolidMasse moléculaire :441.35TD034
CAS :TD034 is a selective, reversible, non-covalent inhibitor of HDAC11, with an IC50 of 5.1 nM and a Ki of 1.5 nM. It does not inhibit other HDACs or sirtuins. TD034 inhibits the desuccinylation of SHMT2 (a substrate of HDAC11) and lowers YAP1 levels by inhibiting HDAC11. TD034 is applicable for lung cancer research.Formule :C45H64N4O6Couleur et forme :SolidMasse moléculaire :757.01PRMT5-IN-21
<p>PRMT5-IN-21 (compound 1) is a potent inhibitor of cyclonucleoside PRMT5.</p>Formule :C18H18F2N6O3Couleur et forme :SolidMasse moléculaire :404.37GSK3368715 dihydrochloride
CAS :GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is a PRMTs inhibitor , with anticancer activity, for the study of advanced solid tumors.Formule :C20H40Cl2N4O2Degré de pureté :99.66% - 99.66%Couleur et forme :SolidMasse moléculaire :439.46LLY-283
CAS :LLY-283, PRMT5 inhibitor, IC50 22 nM, Kd 6 nM, oral, selective, with antitumor effects.Formule :C17H18N4O4Degré de pureté :99.49%Couleur et forme :SolidMasse moléculaire :342.35BAY-3827
CAS :BAY-3827 is an AMPK inhibitor with antiproliferative activity and antitumor activity. BAY-3827 inhibits the phosphorylation of acetyl CoA carboxylase 1.Formule :C27H25FN6ODegré de pureté :99.90%Couleur et forme :SolidMasse moléculaire :468.53YTH-IN-1
CAS :YTH-IN-1 is an inhibitor of the five YTH structural domains in the human.The YTH family of proteins is an N 6-methyladenosine (m6A) reader in gene expression.Formule :C18H24N6O3Degré de pureté :98.46% - 99.94%Couleur et forme :SolidMasse moléculaire :372.42EZM0414
CAS :EZM0414 is a potent, selective, orally bioavailable inhibitor of SETD2 with IC50 of 18 nM in SETD2 biochemical assay and IC50 of 34 nM in a cellular assay.Formule :C22H29FN4O2Degré de pureté :99.58%Couleur et forme :SolidMasse moléculaire :400.49AMG-193
CAS :AMG-193 is an inhibitor of the MTA-PRMT5 complex and is used in the study of cancer, respiratory diseases and digestive disorders.Formule :C22H19F3N4O3Degré de pureté :99.52%Couleur et forme :SolidMasse moléculaire :444.41Pocenbrodib
CAS :<p>Pocenbrodib (FT-7051) is a potent inhibitor of the bromodomain of the CBP/p300 family with potential antitumour activity and is palatable for cancer research.</p>Formule :C28H32FN3O6Degré de pureté :98.48% - 99.54%Couleur et forme :SolidMasse moléculaire :525.57INCB054329
CAS :INCB054329 is a BET inhibitor targeting BRD2/3/4 and BRDT with IC50s ranging from 1-119 nM.Formule :C19H16N4O3Degré de pureté :99.52%Couleur et forme :SolidMasse moléculaire :348.36ORIC-944
CAS :<p>ORIC-944 is an orally available, selective variant of PRC2 with anticancer activity for the study of prostate cancer.</p>Formule :C26H25FN6ODegré de pureté :98.08%Couleur et forme :SolidMasse moléculaire :456.52DN02
<p>DN02: a potent, selective BRD8(1) bromodomain probe; Ki=32 nM; 30x more affine than BRD8(2).</p>Formule :C22H24FN3O3Degré de pureté :98.22% - 99.74%Couleur et forme :SolidMasse moléculaire :397.44BRD0639
CAS :BRD0639 is a first-in-class PRMT5-substrate interaction inhibitor for PBM-dependent PRMT5 activity studies.Formule :C21H22ClN5O4SDegré de pureté :99.85%Couleur et forme :SolidMasse moléculaire :475.95JDTic
CAS :JDTic, a 4-phenylpiperidine derivative distantly related to analgesics like meperidine and ketobemidone and more closely to the mu opioid antagonist alvimopan, exhibits a notably long duration of action, maintaining effects in animals for weeks following a single dose. This duration is not due to irreversible binding to the kappa opioid receptor but rather to altered activity of c-Jun N-terminal kinases. As a highly selective antagonist for the κ-opioid receptor, without influencing the μ- or δ-opioid receptors, JDTic has shown potential in animal studies for producing antidepressant and anxiolytic effects. It also demonstrates promise in treating addiction to substances such as cocaine and morphine, distinguishing itself structurally from other kappa antagonists like norbinaltorphimine.Formule :C28H39N3O3Couleur et forme :SolidMasse moléculaire :465.63Sinefungin
CAS :Sinefungin (Adenosyl-Ornithine) is an effective inhibitor of virion mRNA(guanine-7-)-methyltransferase, mRNA(nucleoside-2'-)-methyltransferase, and viralFormule :C15H23N7O5Degré de pureté :98.12%Couleur et forme :SolidMasse moléculaire :381.39(8R,9S)-Talazoparib
CAS :(8R,9S)-Talazoparib is Talazoparib enantiomer , less active than Talazoparib on the inhibition of PARP1 (IC50: 144 nM).Formule :C19H14F2N6OCouleur et forme :SolidMasse moléculaire :380.35EHMT2-IN-2
CAS :EHMT2-IN-2 Used in the research of blood disease or cancer. EHMT2-IN-2 is a potent EHMT inhibitor, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2.Formule :C21H22N6OCouleur et forme :SolidMasse moléculaire :374.44HJB97
CAS :HJB97 is used for the design of potential PROTAC BET degrader. It also has antitumor activity. HJB97 is a high-affinity inhibitor of BET (Kis: 0.9 nM (BRD2 BD1), 0.27 nM (BRD2 BD2), 0.18 nM (BRD3 BD1), 0.21 nM (BRD3 BD2), 0.5 nM (BRD4 BD1), 1.0 nM (BRD4 BD2), respectively).Formule :C26H28N8O3Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :500.55(3R,4S)-Tofacitinib
CAS :(3R,4S)-Tofacitinib, the less active enantiomer of Tofacitinib, is a JAK3 inhibitor with an IC50 of 1 nM.Formule :C16H20N6ODegré de pureté :98%Couleur et forme :SolidMasse moléculaire :312.37YF-2 hydrochloride
CAS :<p>YF-2 hydrochloride is a potent histone acetyltransferase activator that exhibits high selectivity and can pass through the blood-brain barrier. It specifically acetylates H3 in the hippocampus, with EC50 values of 2.75 μM, 29.04 μM, and 49.31 μM for CBP, PCAF, and GCN5, respectively. Notably, it does not affect HDAC activity. Moreover, YF-2 hydrochloride demonstrates promising anti-cancer and anti-Alzheimer's disease properties.</p>Formule :C20H23Cl2F3N2O3Couleur et forme :SolidMasse moléculaire :467.31Cercosporin
CAS :<p>Cercosporin, produced by the plant pathogen Cercospora kikuchii and the elsinochromes, is a potent photosensitizer with a short activation wavelength. Cercosporin contains perylene quinone structural features essential for PKC activity (IC50: 0.6-1.3 μM).</p>Formule :C29H26O10Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :534.51HIF-PHD-IN-1
CAS :<p>HIF-PHD-IN-1 is a pharmacological compound that acts as an orally active inhibitor of the hypoxia-inducible factor prolyl hydroxylase domain (HIF-PHD), displaying an IC50 of 54 nM for hHIF-PHD2. Its potential as a therapeutic agent for renal anemia is highly promising.</p>Formule :C17H12Cl2N6O3Couleur et forme :SolidMasse moléculaire :419.22BD-9136
BD-9136, a highly selective BRD4 degrader, demonstrates the capability to inhibit tumor growth without inducing adverse effects in mice, showing potential forFormule :C44H44N10O5SDegré de pureté :98%Couleur et forme :SolidMasse moléculaire :824.9520-HETE
CAS :<p>20-HETE is a CYP450 product, vasoconstrictor, modulates K+ channels, affects NADPH, ROS, NF-κB, NO synthase, and cell apoptosis/proliferation.</p>Formule :C20H32O3Degré de pureté :99.79%Couleur et forme :SolidMasse moléculaire :320.47PLK1-IN-6
<p>PLK1-IN-6: potent, selective PLK1 inhibitor, IC50 = 0.45 nM, hinders cancer cell growth.</p>Formule :C28H37N9O3Couleur et forme :SolidMasse moléculaire :547.65CARM1-IN-1 hydrochloride
CAS :CARM1-IN-1 hydrochloride is a potent and selective inhibitor of CARM1 (IC50: 8.6 μM) with minimal inhibition of PRMT1 and SET7.Formule :C26H22Br2ClNO3Couleur et forme :SolidMasse moléculaire :591.72Amredobresib
CAS :Amredobresib is a potent BET inhibitor that impedes the interaction between bromodomains and acetylated lysines on histone H3 and H4, thereby serving as crucial regulators of gene transcription. It proves valuable in the investigation of acute myeloid leukemia (AML) and cancer.Formule :C26H29N9Couleur et forme :SolidMasse moléculaire :467.581Desidustat
CAS :<p>Desidustat is an inhibitor of HIF hydroxylase.</p>Formule :C16H16N2O6Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :332.31Ref: TM-T5176
Produit arrêtéCTB
CAS :<p>CTB (Cholera Toxin B subunit) is an activator of p300 histone acetyltransferase and induces apoptosis in MCF-7 cells.</p>Formule :C16H13ClF3NO2Degré de pureté :99.82%Couleur et forme :SolidMasse moléculaire :343.73PF-03814735
CAS :PF-03814735 is a novel, potent and reversible inhibitor of Aurora A/B with IC50of 0.8 nM/5 nM, is less potent to Flt3, FAK, TrkA, and minimally active to Met and FGFR1. Phase 1.Formule :C23H25F3N6O2Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :474.48BET-IN-15
CAS :<p>BET-IN-15 (compound 1) is a potent, orally active inhibitor of BET, demonstrating inhibitory IC50 values of 0.64 nM for BRD4-BD1 and 0.25 nM for BRD4-BD2.</p>Formule :C21H18F2N4O3SDegré de pureté :98%Couleur et forme :SolidMasse moléculaire :444.45AMPK activator C2
CAS :AMPK activator C2 is an AMPK allosteric activator.Formule :C7H6NO6PDegré de pureté :98%Couleur et forme :SolidMasse moléculaire :231.1Bisindolylmaleimide I HCl
CAS :Bisindolylmaleimide I HCl is a specific ATP-competitive PKC inhibitor.Formule :C25H25ClN4O2Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :448.95JAK2-IN-9
CAS :<p>Compound A8, known as JAK2-IN-9, is a selective JAK2 inhibitor with an IC50 of 5 nM.</p>Formule :C20H24N6O2SDegré de pureté :98%Couleur et forme :SolidMasse moléculaire :412.51BLL5 Maleate
CAS :BLL5 Maleate is a first-in-class selective PRMT5 inhibitor, it blocks EBV-driven B lymphocyte transformation and survival while leaving normal B cells unaffected.Formule :C21H21N3Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :315.41Igermetostat
CAS :<p>Igermetostat, an EZH2 inhibitor, is utilized both in vivo and in vitro for cancer research [1].</p>Formule :C32H46N4O4Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :550.73STAT3-IN-18
CAS :<p>STAT3-IN-18 (compound SPP), a platinum (IV) complex featuring an axial ligand from sandalwood, suppresses the JAK2-STAT3 pathway in breast cancer (BC) cells and</p>Formule :C18H24Cl2N2O6PtDegré de pureté :98%Couleur et forme :SolidMasse moléculaire :630.38BAZ2-ICR
CAS :<p>BAZ2-ICR is an epigenetic chemical probe and it also is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor with IC50s of 130 nM and 180 nM, and Kds of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains.</p>Formule :C20H19N7Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :357.41JAK1-IN-10
CAS :<p>JAK1-IN-10 (compound 9), a cyano-substituted cyclic hydrazine derivative, functions as a potent and selective inhibitor of JAK1 [1].</p>Formule :C15H17N7Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :295.34JAK-IN-34
CAS :<p>JAK-IN-34 (compound 11n) is a potent inhibitor of Janus kinases (JAKs), demonstrating IC50 values of 0.40 nM for JAK1, 0.83 nM for JAK2, 2.10 nM for JAK3,</p>Formule :C27H26N6ODegré de pureté :98%Couleur et forme :SolidMasse moléculaire :450.53JAK1-IN-11
CAS :<p>JAK1-IN-11 (compound 11) serves as a potent inhibitor of Janus kinases, exhibiting nanomolar inhibitory concentrations with IC50 values of 0.02 nM (JAK1) and 0.</p>Formule :C26H36N6O4SDegré de pureté :98%Couleur et forme :SolidMasse moléculaire :528.67Antitumor agent-104
CAS :<p>Antitumor Agent-104 (Compound 9) serves as an antineoplastic by impeding DNA repair mechanisms in tumor cells, primarily through the inhibition of PARP1 enzyme</p>Formule :C31H33FN6O3Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :556.63JAK-IN-27
CAS :<p>JAK-IN-27, also known as compound 1, is an orally active, potent inhibitor of the JAKS family kinases, displaying inhibitory concentrations (IC50s) of 3.0 nM</p>Formule :C20H21F2N7ODegré de pureté :98%Couleur et forme :SolidMasse moléculaire :413.42BBDDL2059
CAS :<p>BBDDL2059 is a selective covalent inhibitor targeting EZH2, exhibiting an IC50 of 1.5 nM against the EZH2-Y641F mutant.</p>Formule :C27H36N4O4SDegré de pureté :98%Couleur et forme :SolidMasse moléculaire :512.66BET-IN-14
CAS :<p>BET-IN-14 is a pan BET inhibitor with an IC50 of 5.35 nM, demonstrating oral activity and anticancer properties [1].</p>Formule :C30H37N7O2Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :527.66Lerzeparib
CAS :<p>Lerzeparib is a PARP (ADP-ribose polymerase) inhibitor that exhibits antineoplastic activity [1].</p>Formule :C21H20FN3O2Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :365.4DPP
CAS :<p>DPP, a Platinum(IV) complex with a pterostilbene-derived axial ligand, inhibits the JAK2-STAT3 pathway in breast cancer (BC) cells, demonstrating</p>Formule :C36H40Cl2N2O10PtDegré de pureté :98%Couleur et forme :SolidMasse moléculaire :926.7BB-Cl-Amidine hydrochloride
CAS :BB-Cl-Amidine hydrochloride is an inhibitor of peptidylarginine deminase (PAD) [1].Formule :C26H27Cl2N5ODegré de pureté :98%Couleur et forme :SolidMasse moléculaire :496.43PARP7-IN-16 free base
CAS :<p>PARP7-IN-16 free base is the freebase form of PARP7-IN-16. As a selective oral inhibitor of PARP-1/2/7, it demonstrates IC50 values of 0.94, 0.87, and 0.21 nM, respectively. This compound is utilized in the research of breast and prostate cancer.</p>Formule :C25H27FN4O4Couleur et forme :SolidMasse moléculaire :466.50BET BD2-IN-3
CAS :<p>BET BD2-IN-3 (compound I-58), a BET inhibitor specifically targeting the BD2 domain, can be radiolabeled with [11C] for use in positron emission tomography (PET) imaging. PET studies with [11C]BD2-IN-3 in mice have demonstrated appropriate biodistribution in peripheral organs and tissues.</p>Formule :C29H30N4OCouleur et forme :SolidMasse moléculaire :450.58
