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"
2613 produits trouvés pour "Chromatine/Épigénétique"
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SGC3027
SGC3027 is an inhibitor of histone methyltransferase,also is a first potent, selective and cell active chemical probe for PRMT7.Formule :C41H47ClN6O6SDegré de pureté :98%Couleur et forme :SolidMasse moléculaire :787.37PROTAC PARP1 degrader-1
PROTACPARP1 degrader-1 (Compound CN0) serves as a PROTAC degrader of PARP1. It activates the cGAS/STING immune pathway, ultimately enhancing T cell-mediated tumor cell killing. PROTACPARP1 degrader-1 inhibits DNA damage repair, leading to the efficient accumulation of cytoplasmic DNA fragments.Formule :C32H28N6O5Masse moléculaire :576.21212PROTAC BRD4 Degrader-15
CAS :PROTAC BRD4 Degrader-15 targets von Hippel-Lindau and BRD4 with IC50s 7.2/8.1 nM and degrades BRD4 in cancer cells.Formule :C57H62F2N10O10S2Couleur et forme :SolidMasse moléculaire :1149.3SJ10542
CAS :SJ10542: potent JAK2/3-targeting PG-PROTAC; DC50s: JAK2 - 14 nM, JAK3 - 11 nM, JAK2-fusion ALL - 24 nM; CRBN recruiter.Formule :C41H46N12O5SCouleur et forme :SolidMasse moléculaire :818.95(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine
CAS :(S,R,S)-AHPC-C2-amide targets Smad3 degradation and boosts HIF-α; it has anti-fibrotic and renal protective roles.Formule :C41H46N6O6SCouleur et forme :SolidMasse moléculaire :750.91HDAC6 degrader-3
CAS :HDAC6 degrader-3: potent, selective, degrades HDAC6 at 19.4 nM, weakens HDAC1 at 0.647 μM, induces α-tubulin hyperacetylation.Formule :C41H41F4N7O11Couleur et forme :SolidMasse moléculaire :883.8BRD4 degrader-6
CAS :BRD4 degrader-6 is a dimeric BDR4PROTAC class degrader with a DC50 of less than 0.1 μM. It effectively induces the ubiquitination and degradation of BDR4, exhibiting anticancer properties.Formule :C61H71BClN9O7S2Couleur et forme :SolidMasse moléculaire :1152.67dBRD9
CAS :dBRD9 is a PROTAC.Formule :C40H45N7O10Degré de pureté :99.81%Couleur et forme :SolidMasse moléculaire :783.83Ref: TM-T31221
1mg129,00€5mg311,00€10mg502,00€25mg874,00€50mg1.320,00€100mg1.833,00€1mL*10mM (DMSO)434,00€Ep300/CREBBP-IN-2
CAS :Ep300/CREBBP-IN-2: Potent, oral Ep300 & CREBBP inhibitor; IC50s: 0.052μM & 0.148μM; cancer research.Formule :C26H27F3N4O4Couleur et forme :SolidMasse moléculaire :516.51HSP70/SIRT2-IN-1
HSP70/SIRT2-IN-1 (Compound 2a) serves as a dual inhibitor targeting both SIRT2 and HSP70, exhibiting an IC50 of 17.3±2.0 μM against SIRT2.Degré de pureté :98%Couleur et forme :Odour SolidPROTAC BRD4 Degrader-2
CAS :PROTAC BRD4 Degrader-2 is an efficacious degrader of PROTAC BRD4(BRD4 BD1,IC50 of 14.2 nM).Formule :C40H39N9O7Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :757.79DNMT2-IN-2
DNMT2-IN-2 is a selective inhibitor of DNA methyltransferase 2 (DNMT2) with a KD value of 3.04 μM. It targets a concealed allosteric binding site of DNMT2 and reduces m5C levels in tRNA of MOLM-13 cells. This compound works synergistically with Doxorubicin to impair cell viability and is applicable in cancer research, including studies of cervical cancer and leukemia.Couleur et forme :Odour SolidHDAC6-IN-61
HDAC6-IN-61 (Compound 4e) is an HDAC6 inhibitor with an IC50 of 73 nM, demonstrating greater selectivity compared to other HDAC isomers. It also acts as an activator of GPR40. HDAC6-IN-61 can increase the acetylation of tubulin and phosphorylation levels of ERK. This compound is relevant for studying neuroinflammation, including Alzheimer's disease.Couleur et forme :Odour SolidXYD190
XYD190 (Compound 14g) is an orally active degrader of CBP/p300. It inhibits the bromodomain of CBP/p300 with an IC50 of 483.7 nM and demonstrates antitumor activity against acute myeloid leukemia.Formule :C55H50F2N10O7Masse moléculaire :1000.3832PROTAC SMARCA2 degrader-19
CAS :PROTAC SMARCA2 degrader-19 (Compound 46) acts as a degrader of SMARCA2, demonstrating degradation capabilities in A549 and MV411 cells with a DC50 of less than 100 nM. Additionally, this compound degrades SMARCA4 in MV411 cells, but with a significantly higher DC50 of over 1000 nM.Formule :C50H58N10O5SCouleur et forme :SolidMasse moléculaire :911.13Fluorescein-NAD+
Fluorescein NAD+ is a non-radioactive PARP assay substrate, enabling direct enzyme measurement by fluorescence. Comes as 81μg in 250μl water.Couleur et forme :SolidMS8511 HCl
MS8511 HCl is a G9a/GLP inhibitor with anticancer activity that can be used in the study of a variety of cancers including brain cancer.Formule :C28H42ClN5O3Degré de pureté :98.9% - 98.96%Couleur et forme :SolidMasse moléculaire :532.12PRMT5-IN-36
CAS :PRMT5-IN-36 (compound 4), an orally active PRMT5 inhibitor, is utilized in cancer research studies.Formule :C20H15F3N6O2Masse moléculaire :428.37PROTAC SMARCA2/4-degrader-28
CAS :PROTAC SMARCA2/4-degrader-28 (PROTAC 1) functions as a partial degrader of SMARCA2 and SMARCA4 through the PROTAC-based mechanism.Formule :C54H68ClN9O11S2Couleur et forme :SolidMasse moléculaire :1118.75TP-472N
CAS :TP-472N serves as a negative control probe for TP-472, which is a specific and effective BRD7/9 probe.Formule :C19H18N2O2Couleur et forme :SolidMasse moléculaire :306.36Anemonin (6CI)
CAS :Anemonin, a furanone dimer from Buttercups, may help manage melanocytes and osteoarthritis.Formule :C10H8O4Couleur et forme :SolidMasse moléculaire :192.17PRMT5-IN-4
CAS :PRMT5-IN-4 (compound AAA-1) is a PRMT5 inhibitor.Formule :C11H13N3O4SCouleur et forme :SolidMasse moléculaire :283.3AUR1545
CAS :AUR1545 is a selective KAT2A/KAT2B degradator, inhibitory against AML, SCLC, and NEPC, and suppressing tumour growth in the NCI-H1048 xenograft model.Formule :C41H50BrN9O5Degré de pureté :98.84%Couleur et forme :SolidMasse moléculaire :828.8GSK973
CAS :GSK973 is a selective oral BET inhibitor, 1600x more for BRD4 BD2 (pIC50 7.8, pKd 8.7) than BD1, effective against other BD2s.
Formule :C23H23FN2O4Couleur et forme :SolidMasse moléculaire :410.445SAMβA TFA
SAMβA TFA, a selective antagonist of Mfn1-βIIPKC association conjugated to the cell permeable peptide TAT47-57, is a rationally designed inhibitor that improvesFormule :C50H73N17O16·xC2HF3O2Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :1168.22 (free acid)PROTAC BRD4 Degrader-8
PROTAC BRD4 Degrader-8: BRD4 inhibitor with IC50s of 1.1/1.4 nM for BD1/BD2, degrades BRD4 in PC3 cells.Couleur et forme :LiquidKiss2 peptide acetate
Kiss2 peptide acetate is the acetate form of Kiss2 peptide, serving as a positive regulator of reproduction. It binds to its homologous receptor Kiss2R (GPR54) in COS-7 cells, activating the PKA and PKC signaling pathways through Gas and Gaq proteins. This activation enhances the activity of both cAMP response element-dependent luciferase (CRE-luc) and serum response element-dependent luciferase (SRE-luc).Formule :C63H84N16O12·xC2H4O2Couleur et forme :SolidMasse moléculaire :1257.44 (free base)GSK232
CAS :GSK232 is a highly selective and cellularly penetrant inhibitor of CECR2 with outstanding physicochemical properties.Formule :C21H27ClN6O3SCouleur et forme :SolidMasse moléculaire :479.0R8-T198wt
CAS :Cell-permeable peptide blocking Pim-1 kinase, halts DU145 cell growth, causes G1 arrest and apoptosis, inert to RPWE-1 cells at 10-20 μM.Formule :C111H211N59O26SDegré de pureté :98%Couleur et forme :SolidMasse moléculaire :2820.33Eldocasiran
CAS :Eldocasiran, a micro-RNA-193a-3p analogue, exhibits anticancer properties. It is utilized in cancer research [1].Formule :C423H529N161O305P42Couleur et forme :SolidMasse moléculaire :14049.5PROTAC BRD9-binding moiety 5
CAS :PROTAC BRD9 binder moiety 5 selectively binds BRD9 with IC50 4.20μM, used in PROTAC synthesis, shows cancer cell antiproliferative activity.Formule :C19H18N6OCouleur et forme :SolidMasse moléculaire :346.39CBP/p300-IN-14
CAS :CBP/p300-IN-14, patent WO2021213521A1's compound 27, inhibits CBP/EP300 with 3.3 nM IC50.Formule :C30H31F2N7O2Couleur et forme :SolidMasse moléculaire :559.622K-252b
CAS :K-252b, an indolocarbazole derived from the actinomycete Nocardiopsis, functions as a protein kinase C (PKC) inhibitor.
Formule :C26H19N3O5Degré de pureté :98%Couleur et forme :Ready-To-Use SolutionMasse moléculaire :453.45BRD4 Inhibitor-27
CAS :BRD4 Inhibitor-27 is a potent BRD4 inhibitor that inhibits BRD4 BD1 and BRD4 BD2 with IC50s of 9.6 and 11.3 μM, respectively.BRD4 Inhibitor-27 has anticancer
Formule :C16H13F3N6Degré de pureté :99.22%Couleur et forme :SolidMasse moléculaire :346.31S-Ruxolitinib
CAS :S-Ruxolitinib can be used in related research in the field of life sciences. Its product number is T3066 and CAS number is 1160597-27-2.
Formule :C17H18N6Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :306.37PRO-HD2
PRO-HD2 is a selective, PROTAC-based degrader of HDAC6 [1].Degré de pureté :98%Couleur et forme :Odour SolidCAY10591
CAS :SIRT1 activated by CAY10591, mimics caloric restriction, extends lifespan, inhibits apoptosis, suppresses TNF-α, and promotes fat mobilization.
Formule :C20H25N5O2Couleur et forme :SolidMasse moléculaire :367.44JHDM-IN-1
CAS :JHDM-IN-1 inhibits JHDMs; IC50: 3.4 μM JMJD2C, 4.3 μM JMJD2A, 5.9 μM JMJD2E, 10 μM PHF8, 43 μM JMJD3.Formule :C27H29N3O6Couleur et forme :SolidMasse moléculaire :491.54CB1R/AMPK modulator 1
Compound 38-S is an orally active CB1R/AMPK modulator with a K i of 0.81 nM and an IC50 of 3.9 nM for CB1R.Formule :C25H22Cl2N6O3SDegré de pureté :98%Couleur et forme :SolidMasse moléculaire :557.45CREBtide
CAS :CREBtide is a synthetic substrate for PKA (Km=3.9 µM), which is based on the phosphorylation sequence in d-CREB (cAMP response element binding protein).Formule :C73H129N29O19Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :1716.99SR-0813
CAS :SR-0813 is a potent and selective inhibitor of the YEATS domain in ENL/AF9.Formule :C25H32N6O3SDegré de pureté :98.81%Couleur et forme :SolidMasse moléculaire :496.62Ref: TM-T40229
1mg39,00€5mg86,00€10mg124,00€25mg253,00€50mg384,00€100mg532,00€200mg705,00€1mL*10mM (DMSO)94,00€ZLN 024 hydrochloride
CAS :ZLN 024 hydrochloride is an AMPK allosteric activator and stimulates the inactive α1 subunit truncations α1 (1-394) and α1 (1-335) but not α1 (1-312).Formule :C13H14BrClN2OSDegré de pureté :98.541%Couleur et forme :SolidMasse moléculaire :361.68PROTAC BRD4 Degrader-28
PROTAC BRD4 Degrader-28 (Compound 4) is a PROTAC degrader specifically targeting BRD4, and it holds potential for cancer research.Formule :C38H36ClN7O8SCouleur et forme :SolidMasse moléculaire :786.25dAURK-4
CAS :dAURK-4, a derivative of Alisertib, functions as a potent and selective degrader of AURKA (Aurora A), exhibiting anticancer properties [1].Formule :C52H52ClFN8O12Couleur et forme :SolidMasse moléculaire :1035.47TDI-012804
TDI-012804 is a TNKS2 inhibitor that selectively inhibits endogenous TNKS2 protein within cells. It enhances the expression of AXIN1 protein in Tnks1 heterozygous (Tnks1HET) and knockout (Tnks1KO) cells. TDI-012804 suppresses the proliferation of ApcQ1405X/Tnks1KO organoids with an EC50 of 59.1 nM and exhibits selective toxicity towards Tnks1KO AKP-G12D and AKP-G13D organoids.Couleur et forme :Odour SolidZIP
CAS :Novel inhibitor for PKMζ, halts synaptic potentiation and reverses LTP with IC50 of 1-2.5 μM, erasing spatial memory.Formule :C90H154N30O17Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :1928.4CBB1007 trihydrochloride (1379573-92-8 free base)
CAS :CBB1007 trihydrochloride is a selective, reversible, and substrate competitive LSD1 inhibitor (IC50: 5.27 μM for hLSD1).Formule :C27H37Cl3N8O4Degré de pureté :98%Couleur et forme :SoildMasse moléculaire :644.0Ref: TM-T10699L2
2mg131,00€5mg187,00€10mg283,00€50mg665,00€100mg1.034,00€200mgÀ demander500mgÀ demander1mL*10mM (DMSO)264,00€SAH-EZH2
CAS :EZH2/EPP inhibitor, Kd 320 nM. Reduces EZH2, H3K27me3; halts MLL-AF9 leukemia growth; drives monocyte-macrophage differentiation.Formule :C155H256N48O40Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :3432.05PROTAC EED degrader-1
PROTAC EED degrader-1 is a PROTAC targeting EED (pKD = 9.02), is a inhibitor of polycomb repressive complex 2 (PRC2) with pIC50 of 8.17.Formule :C55H60FN11O8SDegré de pureté :98%Couleur et forme :SolidMasse moléculaire :1054.2Protein kinase C α peptide TFA
CAS :Protein Kinase C (alpha) Peptide (TFA) is a PKC-α-associated peptide functioning as a lipid-dependent serine/threonine protein kinase.Formule :C68H115F3N24O26SCouleur et forme :SolidMasse moléculaire :1773.85GNE-987
CAS :GNE-987 is a potent chimeric BET degrader, binding BRD4 BD1/BD2 at IC50: 4.7/4.4 nM & has a DC50: 0.03 nM in EOL-1 AML cells.Formule :C56H67F2N9O8S2Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :1096.31GSK 591 dihydrochloride
CAS :Strong PRMT5 inhibitor with 4 nM IC50, surpassing other PRMTs; halts MCL growth in lab tests.Formule :C22H30Cl2N4O2Couleur et forme :SolidMasse moléculaire :453.41JPS036
CAS :JPS036, a benzamide-based VHL E3-ligase PROTAC, potently degrades HDAC1/2, increasing gene expression and apoptosis in HCT116 cells.Formule :C51H66FN7O7SCouleur et forme :SolidMasse moléculaire :940.18PAD2-IN-2 TFA
PAD2-IN-2 (cis-isomer of 1) TFA is an inhibitor of protein arginine deiminase 2 (PAD2). This molecule features an azobenzene photoswitch, enabling the optical regulation of PAD activity. Additionally, PAD2-IN-2 TFA inhibits the citrullination of histone H3.Formule :C28H27ClF3N7O3Couleur et forme :SolidMasse moléculaire :602.01Protein Kinase C (19-31)
CAS :Protein Kinase C (19-31), a PKC inhibitor derived from PKCa, has a serine at position 25 and tests PKC activity.Formule :C67H118N26O16Degré de pureté :98%Couleur et forme :Lyophilized PowderMasse moléculaire :1543.82PROTAC BRD4 Degrader-30
PROTACBRD4 degrader-30 is an ISOX-DUAL-based PROTAC degrader, targeting BRD4 with an IC50 value of 65 nM. It is used in research studies related to c-Myc oncoproteins and the pathophysiology of cancer cells.Couleur et forme :Odour SolidEXQ-2d
EXQ-2d is an inhibitor of tankyrase, effectively targeting TNKS1 and TNKS2 with IC50 values of 48.8 nM and 13.8 nM (pIC50=7.31 and 7.86), respectively. Additionally, EXQ-2d suppresses the WNT/β-catenin signaling pathway with an IC50 of 515 nM. It demonstrates antiproliferative activity in cancer cells COLO 320DM and RKO, with GI50 values of 4.9 μM and 77 μM, respectively.Formule :C18H17N3O3Couleur et forme :SolidMasse moléculaire :323.35Wnt/β-catenin-IN-5
Wnt/β-catenin-IN-5 (Compound 4) functions as an inhibitor of the Wnt/β-catenin signaling pathway. This compound effectively eradicates colorectal cancer stem cells and inhibits tumor growth by suppressing the Wnt signaling pathway. Additionally, Wnt/β-catenin-IN-5 promotes the degradation of KDM3A and KDM3B.Formule :C33H37N5O10Couleur et forme :SolidMasse moléculaire :663.671,4-DPCA
CAS :1,4-DPCA is an inhibitor of prolyl-hydroxylase with an IC50 of 2.4 µM for collagen hydroxylation in human foreskin fibroblasts and 60 μM for factor inhibitingFormule :C13H8N2O3Degré de pureté :97.77%Couleur et forme :SolidMasse moléculaire :240.21Ref: TM-T21653
5mg49,00€10mg79,00€25mg144,00€50mg222,00€100mg356,00€200mg525,00€500mg837,00€1mL*10mM (DMSO)54,00€HD-TAC7
CAS :HD-TAC7 is a PROTAC degrader targeting HDAC, with IC50 values of 3.6/4.2/1.1 μM for HDAC1/HDAC2/HDAC3. It can reduce the expression of NF-κB p65.Formule :C33H32FN7O7Degré de pureté :99.70%Couleur et forme :SolidMasse moléculaire :657.65INCB059872
CAS :INCB059872: potent, oral, selective LSD1 inhibitor for myeloid leukemia research.Formule :C23H34N2O3Couleur et forme :SolidMasse moléculaire :386.536PROTAC BET degrader-2
CAS :PROTAC BET degrader-2 is a highly potent degrader of Bromodomain and Extra-Terminal (BET) proteins (IC50 of 9.6 nM ).Formule :C41H42N10O6Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :770.84Dot1L-IN-8
Dot1L-IN-8 (Compound 15) is an effective Dot1L inhibitor. It suppresses the viability of HL-60, K562, MV4-11, HH, and KG-1 cells, with IC50 values of 0.45, 1.03, 0.68, 1.66, and 1.12 μM, respectively.Formule :C41H53N7O3SCouleur et forme :SolidMasse moléculaire :723.97TCIP3
CAS :TCIP3 is a bivalent molecular glue (molecular glue) that can simultaneously bind to both p300/CBP and BCL6. It redirects p300 and CBP to activate programmed cell death genes, which are typically repressed by the oncogenic driver BCL6. TCIP3 is useful for studying diffuse large B-cell lymphoma (DLBCL) and is not toxic to untransformed tonsil lymphocytes or fibroblasts.Formule :C58H71ClF2N16O7Couleur et forme :SolidMasse moléculaire :1177.74Bisindolylmaleimide XI hydrochloride
CAS :Bisindolylmaleimide XI hydrochloride (Ro 32-0432) is an orally active pan-PKC inhibitor that inhibits PKCα, PKCβI, PKCβII, and PKCγ.Formule :C28H29ClN4O2Degré de pureté :99.45%Couleur et forme :SolidMasse moléculaire :489.01PROTAC SMARCA2 degrader-20
CAS :PROTAC SMARCA2 degrader-20 (Compound I-40) is a potent degrader of PROTAC SMARCA2, showing potential for cancer research applications.Formule :C55H65N11O5SCouleur et forme :SolidMasse moléculaire :992.24UNC10013
UNC10013 is an allosteric modulator of SETDB1, exhibiting negative allosteric regulation through covalent bond formation with Cys385 on the 3TD domain. It has a kinact/KI value of 1.0 × 10^6 M^-1*s^-1. UNC10013 effectively disrupts SETDB1-mediated Akt methylation, holding potential for application in cancer and neurodegenerative disease research.Couleur et forme :Odour SolidAdenosine receptor modulator 1
Adenosine receptor modulator 1 acts as an inducer of collagen VII (C7). It enhances the expression of COL7A1 mRNA in donor-derived keratinocytes and, in synergy with Gentamicin, increases the overall levels of C7.Formule :C25H28N6O3Couleur et forme :SolidMasse moléculaire :460.53MAT2A-IN-14
MAT2A-IN-14 (compound H3) is a MAT2A inhibitor that generates reactive oxygen species (ROS) following ultrasound treatment, leading to the specific degradation of MAT2A in cells through rapid oxidation reactions. When combined with ultrasound, MAT2A-IN-14 induces an 87% reduction of MAT2A in human colon cancer cells.Formule :C27H24F2N4O4Masse moléculaire :506.17656CEM114
CAS :CEM114 is a potent chemical compound known as a chemical epigenetic modifier (CEM).Formule :C84H122FN9O19SCouleur et forme :SolidMasse moléculaire :1613.0mUNO
CAS :mUNO is a tumor-homing peptide (mUNO, sequence: "CSPGAK") that specifically binds to murine CD206, targeting tumor-associated macrophages that express CD206/MRC1. Additionally, mUNO can interact with human recombinant CD206.Formule :C22H39N7O8SCouleur et forme :SolidMasse moléculaire :561.652MD6a
MD6a is a melatonin derivative with inhibitory activity against poly(ADP-ribose) polymerase (PARP-1). It maintains protein homeostasis and improves mitochondrial function via the TOR/HSF-1 signaling pathway, providing neuroprotective effects.Formule :C21H22N2O2Masse moléculaire :334.16813UNC4976
UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids.Formule :C47H70N6O8Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :847.09TYK2 activator-1
TYK2activator-1 (16b) is a TYK2 activator with an EC50 value of 1.78 μM. It inhibits JAK2 and JAK3 with IC50 values of 6.8 μM and 6.3 μM, respectively.Formule :C23H21FN4O2Couleur et forme :SolidMasse moléculaire :404.16485Menin-KMT2A-IN-1
Menin–KMT2A-IN-1 (Compound 20) is an inhibitor of menin–KMT2A, binding to menin with an IC50 of 8 nM, and disrupting the interaction between menin and lysine methyltransferase 2A (KMT2A). It inhibits hERG channels with an IC50 of 65 μM and suppresses MV4-11 cells with an IC50 of 74 nM. Furthermore, Menin–KMT2A-IN-1 exhibits favorable pharmacokinetic properties in CD-1 mice, with an oral bioavailability of 74%.Formule :C28H35FN6O3Couleur et forme :SolidMasse moléculaire :522.61PROTAC Sirt2 Degrader-1
CAS :PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and aFormule :C40H40N10O8S2Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :852.94Izilendustat
CAS :Tert-butyl compound inhibits human EGLN-1; confirmed by spectrometry after 20 mins.Formule :C22H28ClN3O4Degré de pureté :99.95%Couleur et forme :SolidMasse moléculaire :433.93Ref: TM-T64336
5mg43,00€10mg60,00€25mg103,00€50mg166,00€100mg259,00€200mg378,00€1mL*10mM (DMSO)47,00€Cath-L-dBET1
Cath-L-dBET1 is a PROTAC degrader targeting BRD4. It has an IC50 value of 2.8 μM in MDA-MB-231 cells. Activated by cathepsin L (Cath-L), Cath-L-dBET1 recruits E3 ubiquitin ligase to degrade BRD4 via the ubiquitin-proteasome system. Hyp-dBET1 is applicable for antitumor research.Couleur et forme :Odour Solid(rel)-Tranylcypromine D5 hydrochloride
CAS :(rel)-Tranylcypromine D5 hydrochloride is a deuterium labeled (rel)-Tranylcypromine hydrochloride.Formule :C9H12ClNDegré de pureté :98%Couleur et forme :SolidMasse moléculaire :174.682JQ-1 (carboxylic acid)-NH-C2-NH-AMPRO-222
JQ-1 (carboxylic acid)-NH-C2-NH-AMPRO-222 incorporates a BRD4 ligand and a PROTAC linker, and is used in the synthesis of PROTAC BRD4 Degrader-29.
Formule :C43H51ClN8O3S2Couleur et forme :SolidMasse moléculaire :827.5MACTIDE-V
MACTIDE-V is an orally active and selective peptide-drug conjugate targeting CD206. This compound delivers Verteporfin to CD206+ tumor-associated macrophages (TAM), thereby inhibiting the YAP/TAZ signaling pathway. It facilitates YAP exclusion from the nucleus, induces TAM polarization toward an anti-tumor phenotype, enhances phagocytosis and antigen presentation, and promotes T cell infiltration and NK cell activity. MACTIDE-V suppresses primary tumor growth and lung metastasis in triple-negative breast cancer (TNBC) mouse models.Formule :C109H156N22O27S2Couleur et forme :SolidMasse moléculaire :2269.09517Mz325
CAS :Mz325 serves as a dual inhibitor of both HDAC and Sirt2, exhibiting an IC50 of 9.7 µM against Sirt2, which are implicated in the pathogenesis of cancer andFormule :C38H45N9O5S2Degré de pureté :98.71%Couleur et forme :Odour SolidMasse moléculaire :771.951E67-2
CAS :E67-2: Low-toxic, KIAA1718 inhibitor with IC50 of 3.4μM, targets H3K9/H3K4 demethylases.Formule :C21H36N6O2Couleur et forme :SolidMasse moléculaire :404.559WDR5 ligand 2
CAS :WDR5ligand 2 is a ligand for WDR5 and can be utilized in the synthesis of PROTAC WDR5degrader 1.Formule :C29H31F3N4O4Couleur et forme :SolidMasse moléculaire :556.576Martinostat
CAS :Martinostat is an HDAC inhibitor that can be radiolabeled for quantitative imaging of HDACs within the central nervous system and major peripheral organs.Formule :C22H30N2O2Couleur et forme :SolidMasse moléculaire :354.49SIRT-IN-5
SIRT-IN-5, a selective inhibitor of SIRT3 with an IC50 of 2.88 μM, facilitates the differentiation of multiple myeloma cells. This differentiation is associated with increased expression of the differentiation antigens CD49e and human immunoglobulin light chains λ and κ.Couleur et forme :Odour SolidUNC2399
CAS :UNC2399, a biotinylated version of UNC1999, functions as a selective degrader of EZH2 and exhibits strong in vitro efficacy against EZH2, demonstrated by its IC
Formule :C67H104N10O17SCouleur et forme :SolidMasse moléculaire :1353.68Aurothiomalate tetramer sodium
Aurothiomalate tetramer sodium, a tetrameric form of Aurothiomalate sodium, functions as an anti-arthritis gold agent. It also acts as a potent and selective inhibitor of the oncogenic PKCι signaling pathway.Couleur et forme :Odour SolidHIF1-IN-3
CAS :HIF1-IN-3 (Benzenepropanamide, N-[(8-hydroxy-7-quinolinyl)(4-methoxyphenyl)methyl]-) is an effective inhibitor of HIF-1 (EC50 = 0.9 μM) and can be used inFormule :C26H24N2O3Degré de pureté :99.59%Couleur et forme :SolidMasse moléculaire :412.48coumarin-SAHA
CAS :SAHA inhibits class I/II HDAC; c-SAHA, a fluorescent derivative, excites at 325 nm and emits at 400 nm.Formule :C18H22N2O5Couleur et forme :SolidMasse moléculaire :346.383BI01826025
BI01826025 (pArg-JQ1), a BRDT BD1 bromodomain PROTAC degrader, tests ClpC2's effect on ClpC1P1P2 protease.Formule :C31H42ClN10O7PSCouleur et forme :SolidMasse moléculaire :765.22SMD-3236
CAS :SMD-3236 is a PRAOTAC degrader targeting SMARCA2, designed using SMARCA ligand and VHL-1 ligand, and exhibits prolonged anti-tumor activity in vivo. SMARCA2 acts as a synthetic lethal target in cancer cells lacking SMARCA4, with SMD-3236 showing 2000-fold selectivity for SMARCA2 over SMARCA4, having a DC50 of less than 1 nM and a Dmax of over 95%. In the human cancer xenograft models deficient in SMARCA4, notably the H838 model, SMD-3236 effectively induces loss of SMARCA2 in tumor tissue while sparing the SMARCA4 protein, thereby inhibiting tumor growth. The compound consists of a target protein ligand (red part) SMI-1074, a PROTAC linker (black part) (trans-4-Ethynylcyclohexyl)methyl methanesulfonate, and an E3 ligase ligand (blue part) SMARCA2 ligand-14, forming the E3LigaseLigand-linker Conjugate 159.Formule :C61H75ClN10O5SCouleur et forme :SolidMasse moléculaire :1095.83Dihydrochlamydocin
CAS :Dihydrochlamydocin, an inhibitor of histone deacetylases (HDAC), exhibits potent cytostatic activity against mastocytoma cells.Formule :C28H40N4O6Couleur et forme :SolidMasse moléculaire :528.65iRucaparib-AP6
CAS :iRucaparib-AP6: a specific, non-trapping PARP1 degrader; inhibits the enzyme's activity and scaffolding.Formule :C46H55FN6O11Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :886.96PARP/HDAC-IN-1
PARP/HDAC-IN-1 is a PARP and HDAC inhibitor that inhibits PARP1, PARP2, and HDAC1, and may be used to study pancreatic cancer.Formule :C36H32F2N6O3Degré de pureté :95.00%Couleur et forme :SolidMasse moléculaire :634.67HDAC1-IN-9
HDAC1-IN-9 (13c) is an HDAC1 inhibitor. It inhibits the HDAC1 enzyme with an IC50 value of 1.07 µM. This compound exhibits the strongest antiproliferative activity against HT-29 (human colon adenocarcinoma cells), with an IC50 of 1.78 μM. In HCT-116 (human colon cancer cells), HDAC1-IN-9 significantly induces apoptosis. Additionally, HDAC1-IN-9 possesses antiangiogenic properties, reducing the expression levels of VEGFR-2 and phosphorylated VEGFR-2 (pVEGFR-2) by approximately 80%.Formule :C17H17N3O3Couleur et forme :SolidMasse moléculaire :311.34DW71177
CAS :DW71177 is a BET inhibitor with potent anti-leukemic activity for the study of leukemia.Formule :C20H28N6O2Degré de pureté :98.13%Couleur et forme :SoildMasse moléculaire :384.48HDAC-IN-89
HDAC-IN-89 is an inhibitor of HDAC1 (IC50: 0.95 nM), HDAC2 (IC50: 0.86 nM), HDAC3 (IC50: 1.06 nM), and HDAC8 (IC50: 4.24 nM). It can disrupt the cell cycle and induce apoptosis. Additionally, HDAC-IN-89 exhibits antitumor activity.
Couleur et forme :Odour SolidPAD2-IN-1
CAS :PAD2-IN-1 is a selective benzimidazole-derived inhibitor with a 95-fold and 79-fold higher affinity for PAD2 over PAD4 and PAD3, respectively.Formule :C25H29FN6O3Couleur et forme :SolidMasse moléculaire :480.544WQQ-345
WQQ-345, a BCAT1 inhibitor, exhibits an IC50 of 10.8 mM. In 67R cells, it reduces α-KG levels and upregulates H3K27me3 expression while downregulating the expression of glycolytic enzymes (PFKP and LDHA), leading to impaired glycolytic activity. Additionally, WQQ-345 demonstrates tumor-suppressive activity in a 67R subcutaneous xenograft model.Formule :C10H17NO2Couleur et forme :SolidMasse moléculaire :183.25
