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.

Signaling Pathways

Product Type

Histone Methyltransferase Histone methyltransferase

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