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Histone Methyltransferase Histone methyltransferase

Inhibitors

Cat.No.  Name Information
M21507 AS-99 TFA AS-99 TFA is the first-in-class, effective and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemia activity. In vivo, AS-99 TFA blocked cell proliferation, induced apoptosis and apoptosis, down-regulated MLL fusion target genes, and alleviated leukaemia.
M21505 AS-99 AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with antileukemic activity.
M21504 AS-99 free base AS-99 is the first-in-class, effective and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemia activity.
M21488 CM-579 CM-579 is a first-in-class reversible dual inhibitor of G9a and DNA methyltransferase (DNMT) with IC50 values of 16 nM and 32 nM, respectively. It plays an active role in a variety of cancer cells.
M21487 Valemetostat tosylate Valemetostat tosylate (DS-3201 tosylate) is a first-in-class EZH1/2 inhibitor with IC50 < 10 nM. Valemetostat tosylate can be used in the study of relapsed and refractory peripheral T cell lymphoma.
M21486 CM-579 trihydrochloride CM-579 trihydrochloride is a dual inhibitor of G9a and DNA methyltransferase (DNMT), with IC50 values of 16 nM and 32 nM, respectively, as first-in-class, reversible. It plays an active role in a variety of cancer cells.
M21482 MS117 MS117 is a first-in-class, cell-active, irreversible covalent inhibitor of protein arginine methyltransferase (PRMT6) with an IC50 value of 18 nM.
M21306 UNC6852 UNC6852 is a PROTAC technology-based, selective PRC2 degradation agent containing an EED ligand and a von Hippel-Lindau ligand with an IC50 value of 247 nM for EED action.
M21119 CPI-1328 CPI-1328 is an EZH2 inhibitor with a Ki value of 63 fM.
M21075 PF-06939999 PF-06939999 (PRMT5-IN-3) is a PRMT5 inhibitor that is synthetically lethal to tumor cells in combination with DNA damaging agents.
M20623 LLY-284 LLY-284 is the diastereomer of LLY-283, which is a potent and selective SAM-competitive chemical probe for PRMT5. LLY-284 is much less active than LLY-283 and can be used as a negative control for LLY-283.
M20492 AMI-1, free acid AMI-1 is a potent and specific Histone Methyltransferase (HMT) inhibitor with IC50 of 3.0 μM and 8.8 μM for yeast Hmt1p and human PRMT1, respectively.
M13850 SGC3027 SGC3027 is a histone methyltransferase inhibitor. SGC3027 is the first potent, selective and cell active chemical probe for PRMT7.
M13849 MS023 dihydrochloride MS023 dihydrochloride is a potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases (PRMTs) inhibitor, with IC50s of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively.
M13848 MM-102 TFA MM-102 TFA (HMTase Inhibitor IX TFA) is a potent WDR5/MLL interaction inhibitor, achieves IC50 = 2.4 nM with an estimated Ki < 1 nM in WDR5 binding assay, which is >200 times more potent than the ARA peptide.
M13847 EZM 2302 EZM 2302 is an inhibitor of coactivator-associated arginine methyltransferase 1 (CARM1) with an IC50 of 6 nM.
M13846 EPZ011989 trifluoroacetate EPZ011989 trifluoroacetate is a potent, selective orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 wt and EZH2 Y646; 15-fold selectivity over EZH1 and >3000-fold selectivity over other HMTase.
M13845 CARM1-IN-1 hydrochloride CARM1-IN-1 hydrochloride is a potent and specific CARM1(Coactivator-associated arginine methyltransferase 1) inhibitor with IC50 of 8.6 uM; shows very low activity against PRMT1 and SET7(IC50 > 600 uM).
M13844 CARM1-IN-1 CARM1-IN-1 is a potent and specific CARM1(Coactivator-associated arginine methyltransferase 1) inhibitor with IC50 of 8.6 uM; shows very low activity against PRMT1 and SET7(IC50 > 600 uM).
M13843 BRD9539 BRD9539 is a histone methyltransferase G9a inhibitor with an IC50 of 6.3 μM. BRD9539 also inhibits PRC2 activity and is inactive against SUV39H1, NSD2 and DNMT1.



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