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"
2612 produits trouvés pour "Chromatine/Épigénétique"
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Galegine 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 :225.27PROTAC 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 :297.31Tripolin B
CAS :Tripolin B is an ATP-competitive inhibitor of Aurora kinases, with IC50 values of 2.5 µM and 6 µM for Aurora A and Aurora B kinases, respectively. However, it exhibits no inhibitory effect within cells.Formule :C12H9N3OMasse moléculaire :211.22BET-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 :423.48FT001
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 :467.58Ref: TM-T27392
1mg109,00€2mg163,00€5mg241,00€10mg354,00€25mg532,00€50mg745,00€100mg1.018,00€500mg2.035,00€1mL*10mM (DMSO)284,00€DS17701585
DS17701585: Oral EP300/CBP inhibitor; potent on CBP, EP300, H3K27, & SOX2; useful for cancer research.Formule :C24H26N4O5SCouleur et forme :SolidMasse moléculaire :482.55PROTAC 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 :647.72JTZ-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 :376.79BRD4-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 :527.61BBC0403
CAS :BBC0403 is a BRD2 inhibitor, inhibiting BRD2 and BRD2, and suppresses NF-κB and MAPK signaling pathways.Formule :C21H22N2O5Degré de pureté :98.15%Couleur et forme :SolidMasse moléculaire :382.41Ref: TM-T88118
1mg59,00€5mg124,00€10mg193,00€25mg358,00€50mg512,00€100mg707,00€1mL*10mM (DMSO)131,00€I-BET282E
I-BET282E inhibits eight BET bromodomains (pIC50 6.4-7.7) with selectivity for other bromodomain proteins.Formule :C26H34N4O7SCouleur et forme :SolidMasse moléculaire :546.64CBP/p300-IN-16
CBP/p300-IN-16 (compound 1) is a potent inhibitor of EP300/CBP HAT, acting on HAT EP300 (IC50: 0.61 μM) and LK2 H3K27 (IC50: 2.24 μM).Formule :C26H31N3O4Couleur et forme :SolidMasse moléculaire :449.54NI-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 :488.54HDAC2-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 :426.96PRMT5-MTA-IN-3
CAS :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.Formule :C19H17F3N6O3Couleur et forme :SolidMasse moléculaire :434.372iBRD4-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 :749.62BRD9 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 :760.87PRMT5-IN-44
CAS :PRMT5-IN-44 (compound 12) is an inhibitor of PRMT5, specifically utilized in cancer research.Formule :C23H19F4N5O2Couleur et forme :SolidMasse moléculaire :473.42Streptonigrin (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 :506.46Pociredir
CAS :Pociredir (FTX-6058), a potent EED inhibitor (KD=0.163 nM), may help in SCD research.Formule :C22H18FN5O2Couleur et forme :SolidMasse moléculaire :403.41HDAC-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 :367.44O-Desmethyl Midostaurin
CAS :O-Desmethyl Midostaurin is the active Midostaurin metabolite via cytochrome P450 liver enzyme metabolism.Formule :C34H28N4O4Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :556.61HDAC6-IN-9
CAS :HDAC6-IN-9 is a γ-secretase modulator that can significantly reduce the level of Aβ42 in mouse brain and can be used to study neurological diseases.Formule :C19H16N2O3Degré de pureté :98.84%Couleur et forme :SolidMasse moléculaire :320.34PARP10/15-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 :274.3HIF-1α-IN-4
HIF-1α-IN-4 is an inhibitor of HIF-1α with IC50 of 24 nM in HEK293T cells which has potential antitumor effects.Formule :C16H12N2O3Couleur et forme :SolidMasse moléculaire :280.28Triciferol
CAS :Triciferol is a VDR agonist and HDAC antagonist with 1,25D-like potency, affecting gene targets and tubulin, and shows anti-cancer effects in vitro. IC50=87nM.Formule :C26H39NO4Couleur et forme :SolidMasse moléculaire :429.591CM-414
CAS :CM-414: HDAC/PDE5 inhibitor, targeting Alzheimer’s, IC50s: PDE5 (60 nM), HDAC1/2/3/6. Reduces Aβ, pTau in mice, boosts cognition.Formule :C23H29N5O4Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :439.51LSD1-IN-39
CAS :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.Formule :C25H30N2O7Couleur et forme :SolidMasse moléculaire :470.515RK-582
CAS :RK-582: oral spiroindolinone tankyrase inhibitor, halts colon cancer growth in COLO-320DM mouse model.Formule :C27H35FN6O3Couleur et forme :SolidMasse moléculaire :510.6KH-259
KH-259: potent, selective CNS-penetrant HDAC6 inhibitor with 0.26 μM IC50; shows antidepressant effects in mice.Formule :C20H25N3O2Couleur et forme :SolidMasse moléculaire :339.43AS2521780
CAS :AS2521780 is an inhibitor of PKCθ (IC50: 0.48 nM).Formule :C30H41N7OSDegré de pureté :98%Couleur et forme :SolidMasse moléculaire :547.76TAF1 ligand 1
CAS :TAF1 ligand 1 is a TAF1 ligand. It can serve as a ligand for target proteins (Ligands for Target Protein for PROTAC) in the synthesis of PROTACs targeting TAF1, such as ZS3-046.Formule :C23H23N5O3Couleur et forme :SolidMasse moléculaire :417.46HDAC/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 :401.15869HDAC-IN-32
HDAC-IN-32, potent inhibitor: IC50—HDAC1 (5.2 nM), HDAC2 (11 nM), HDAC6 (28 nM). Effective anti-tumor and immunity-boosting traits.Formule :C20H23N3O3Couleur et forme :SolidMasse moléculaire :353.41NPC26
CAS :NPC26 is a small molecule that disrupts mitochondrial function and exhibits antitumor activity. It shows significant antiproliferative and cytotoxic effects on CRC cell lines (HCT-116, DLD-1, and HT-29). NPC26 induces mitochondrial permeability transition pore (mPTP) opening, generates reactive oxygen species (ROS), and triggers cell death. Additionally, NPC26 kills CRC cells by activating the AMP-activated protein kinase (AMPK) signaling pathway.Formule :C19H23N3O5S2Couleur et forme :SolidMasse moléculaire :437.533iBFAR2
CAS :iBFAR2, an inhibitor of BFAR, restores the CD8+ tumor-resident memory T cell subset against solid tumors. It promotes the binding of JAK2-STAT1 and enhances the phosphorylation of STAT1.
Formule :C19H15F3N2O2Couleur et forme :SolidMasse moléculaire :360.33PF-06726304 acetate
CAS :PF-06726304 acetate is a selective inhibitor of EZH2, with robust antitumor growth activity.Formule :C24H25Cl2N3O5Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :506.38MS8815
CAS :MS8815 is a selective EZH2 PROTAC degrader with IC50 of 8.6 nM, used in triple-negative breast cancer research.Formule :C65H87N9O8SCouleur et forme :SolidMasse moléculaire :1154.51PARP7-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 :545.94AZ0108
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 :500.45RL5a
CAS :RL5a (compound C23) is a novel inhibitor of SETD8.Formule :C17H19N3OCouleur et forme :SolidMasse moléculaire :281.35GDC-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 :465.5TYK2 ligand 2
CAS :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.Formule :C24H20FN7O4Couleur et forme :SolidMasse moléculaire :489.458CARM1-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 :481.46LSD1-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 :554.73WDR5-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 :534.58CFT8634
CAS :CFT8634 degrades BRD9, for synovial sarcoma and SMARCB1 tumor research, from patent WO2021178920A1.Formule :C37H45F3N6O5Couleur et forme :SolidMasse moléculaire :710.79LSD1/2-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 :248.07HDAC-IN-27
HDAC-IN-27 is a potent and orally active inhibitor of HDAC Class I (0.43 nM - 3.01 nM for HDAC1-3).Formule :C20H22N4O2Couleur et forme :SolidMasse moléculaire :350.41AZ13824374
AZ13824374: potent, selective ATAD2 inhibitor; anti-proliferative in breast cancer; pIC50: FRET 8.2, NanoBRET 6.2.Formule :C30H39FN8O2Couleur et forme :SolidMasse moléculaire :562.68AMPK 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 :457.927Itareparib
CAS :Itareparib is a PARP inhibitor with demonstrated antitumor activity.Formule :C20H26FN3O2Couleur et forme :SolidMasse moléculaire :359.438AFM-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 :502.97Tyk2-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 :443.50P300 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 :535.03LSD1-IN-17
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.Formule :C20H18N2OSCouleur et forme :SolidMasse moléculaire :334.43HDAC6-IN-13
HDAC6-IN-13: potent, selective HDAC6 inhibitor; oral; IC50=0.019μM; targets HDAC1/2/3; crosses blood-brain barrier; anti-inflammatory.Formule :C23H22N4OCouleur et forme :SolidMasse moléculaire :370.45MAT2A-IN-17
CAS :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.
Formule :C23H18F3N7OCouleur et forme :SolidMasse moléculaire :465.4315-AIQ hydrochloride
CAS :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.Formule :C9H9ClN2OCouleur et forme :SolidMasse moléculaire :196.634JAK-IN-19
JAK-IN-19 inhibits JAK (pIC50: 7.2, 7.7), less so for VEGFR2 (7.0) and Aurora B (5.8).Formule :C26H36FN5O2Couleur et forme :SolidMasse moléculaire :469.59HDAC6-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 :345.44KDOAM-25 citrate
CAS :KDOAM-25 citrate inhibits KDM5A/B/C/D (IC50: 71, 19, 69, 69 nM); boosts H3K4 methylation, hinders MM1S cell growth. [1]Formule :C21H33N5O9Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :499.51(rac)-Talazoparib
CAS :(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.Formule :C19H14F2N6OCouleur et forme :SolidMasse moléculaire :380.351IBL-302
CAS :IBL-302 (AMU302), an orally available dual-signaling inhibitor targeting PIM and PI3K/AKT/mTOR, is effective against breast cancer and neuroblastoma. It has shown in vivo efficacy in a nude mouse xenograft model by combating trastuzumab resistance. Additionally, IBL-302 augments the effectiveness of widely used cytotoxic chemotherapy drugs such as cisplatin, doxorubicin, and etoposide [1] [2] [3].Formule :C25H18FN5O4S3Couleur et forme :SolidMasse moléculaire :567.64MAT2A-IN-24
CAS :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.Formule :C32H33Cl2N7O2Couleur et forme :SolidMasse moléculaire :618.556PAD4-IN-5
CAS :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).Formule :C34H41N7O3Couleur et forme :SolidMasse moléculaire :595.734DS44470011
CAS :DS44470011 is an inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PHD) with oral bioavailability. It enhances the release of erythropoietin (EPO) from cells and is utilized in research related to renal anemia.Formule :C21H19N3O4Couleur et forme :SolidMasse moléculaire :377.39MAT2A-IN-20
CAS :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.
Formule :C26H24F2N6O4Couleur et forme :SolidMasse moléculaire :522.503Equisetin
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 :373.49GDC-9918
CAS :GDC-9918 (compound GDC-9918) is an inhibitor of Janus kinases.Formule :C20H18F2N6O5SCouleur et forme :SolidMasse moléculaire :492.46Pim-1 kinase inhibitor 6
CAS :Pim-1 kinase inhibitor 6 (Compound 4d) is a robust inhibitor of Pim-1 kinase, demonstrating an IC 50 of 0.46 μM. It significantly exhibits cytotoxic effects on cancer cells [1].Formule :C21H10BrCl2N3Couleur et forme :SolidMasse moléculaire :455.13NSD2-PWWP1-IN-1
CAS :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.Formule :C28H30N4Couleur et forme :SolidMasse moléculaire :422.565(2S,3R)-LP99
CAS :(2S,3R)-LP99 is a less active enantiomer of LP99.Formule :C26H30ClN3O4SDegré de pureté :98%Couleur et forme :SolidMasse moléculaire :516.05B026
CAS :B026: Oral p300/CBP HAT inhibitor, IC50: p300 1.8 nM, CBP 9.5 nM; targets AR+ prostate cancer cells.Formule :C27H23F4N5O4Couleur et forme :SolidMasse moléculaire :557.5JPHM-2-167
CAS :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.Formule :C30H28N6O2Couleur et forme :SolidMasse moléculaire :504.582JAK3-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 :401.46BSI-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 :317.037O6BTG-C8-αGlu
CAS :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.Formule :C24H34BrN5O7SCouleur et forme :SolidMasse moléculaire :616.525MAT2A-IN-21
CAS :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.
Formule :C26H20F2N4O2Couleur et forme :SolidMasse moléculaire :458.459Sapintoxin D
CAS :Sapintoxin D is a fluorescent phorbol ester and selective activator of protein kinase C.Formule :C30H37NO8Couleur et forme :SolidMasse moléculaire :539.62MS117
MS117 is a first-in-class and cell-active irreversible covalent inhibitor of protein arginine methyltransferase 6 (PRMT6) (IC50 = 18 nM) [1].Formule :C17H22N4OCouleur et forme :SolidMasse moléculaire :298.38SMARCA2-IN-6
CAS :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.Formule :C10H8ClF2N5OSCouleur et forme :SolidMasse moléculaire :319.72AR/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 :724.85Balomenib
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 :617.664HIF-1/2α-IN-1
HIF-1/2α-IN-1, an orally active compound, functions as an inhibitor of HIF-2α.Formule :C17H16N6O4Couleur et forme :SolidMasse moléculaire :368.356K465
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 :542.05FNDR-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 :413.9Tyk2-IN-14
CAS :Tyk2-IN-14, a small molecule inhibitor of TYK2, is significant in treating inflammatory diseases and conditions linked to hypersecretion of IFNa and interferons [1].Formule :C22H21N9O2Couleur et forme :SolidMasse moléculaire :443.46EZH2-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 :460.35YEATS4 binder-1
YEATS4 binder-1(4e) is an effective and selective compound that targets the KAc recognition site within the YEATS structural domain, exhibiting a bindingFormule :C23H34N4O3Couleur et forme :SolidMasse moléculaire :414.54Tyk2-IN-17
CAS :Tyk2-IN-17 (compound 185) effectively inhibits TYK2 [1].Formule :C20H20F2N8OCouleur et forme :SolidMasse moléculaire :426.42SE-7552
CAS :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].Formule :C15H12F3N5OCouleur et forme :SolidMasse moléculaire :335.28HDAC/Top-IN-1
CAS :HDAC/Top-IN-1, an oral HDAC/Top inhibitor, targets HDAC1-3,6,8 with low IC50s; blocks S-phase & induces apoptosis in HEL cells.Formule :C29H25FN4O4Couleur et forme :SolidMasse moléculaire :512.53KDOAM-25 trihydrochloride
KDOAM-25 trihydrochloride selectively inhibits KDM5 enzymes, boosts H3K4 methylation, and suppresses MM1S cell growth.Formule :C15H28Cl3N5O2Couleur et forme :SolidMasse moléculaire :416.77MAT2A-IN-18
CAS :MAT2A-IN-18 (Compound 15) is an inhibitor of methionine adenosyltransferase 2A (MAT2A) with an IC50 of 50 nM or less.Formule :C17H13ClN4OCouleur et forme :SolidMasse moléculaire :324.764CRV431
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 :1303.76W4275
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 :468.59JAK2-IN-11
CAS :JAK2-IN-11 (Example 6) is a JAK2 kinase inhibitor with potent antitumor activity, exhibiting an IC50 of ≤10 nM against JH2 BIND WT/V617F. This compound effectively suppresses tumor growth.Formule :C31H31F3N8O4Couleur et forme :SolidMasse moléculaire :639.64MAT2A-IN-16
CAS :MAT2A-IN-16 is a MAT2A inhibitor that effectively suppresses the proliferation of MTAP-/-HCT-116 cells, with an IC50 value of 20 nM.Formule :C23H17ClN6OCouleur et forme :SolidMasse moléculaire :428.874DCHC
CAS :DCHC is an activator of SIRT1, but it does not induce SIRT1 expression. This compound can be utilized in studies related to mitochondrial damage.Formule :C15H8Cl2O3Couleur et forme :SolidMasse moléculaire :307.128
