Histone Methyltransferase

Histone Methyltransferase Related Products (165):

By Effects:	Inhibitors (158) Antagonists (7)

Cat. No.	Product Name	Effect	Purity

HY-13803

Tazemetostat	Inhibitor	≥98.0%
Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat (EPZ-6438) inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a K_i value of 2.5 nM. Tazemetostat (EPZ-6438) inhibits EZH2 with IC₅₀s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat (EPZ-6438) inhibits rat EZH2 with an IC₅₀ of 4 nM. Tazemetostat (EPZ-6438) also inhibits EZH1 with an IC₅₀ of 392 nM.

HY-13470

GSK126	Inhibitor
GSK126 (GSK2816126A) is a potent, highly selective inhibitor of EZH2 methyltransferase with an IC₅₀ of 9.9 nM.

HY-101563

GSK3326595	Inhibitor	≥98.0%
GSK3326595 (EPZ015938) is a potent, selective, reversible inhibitor of protein arginine methyltransferase 5 (PRMT5) with an IC₅₀ of 6.2 nM.

HY-15593

Pinometostat	Inhibitor	99.99%
Pinometostat (EPZ-5676) is a potent DOT1L histone methyltransferase inhibitor with a K_i of 80 pM.

HY-12186

3-Deazaneplanocin A hydrochloride	Inhibitor	99.98%
3-Deazaneplanocin A hydrochloride (DZNep hydrochloride) is a potent histone methyltransferase EZH2 inhibitor. 3-Deazaneplanocin A hydrochlorideis a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor.

HY-138684

MRTX9768	Inhibitor	99.60%
MRTX9768 is a potent, orally active PRMT5 inhibitor. MRTX9768 is a synthetic lethal-based inhibitor binding the PRMT5-MTA complex.

HY-141429A

AS-99 TFA	Inhibitor	98.85%
AS-99 TFA is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC₅₀= 0.79 µM, K_d= 0.89 µM) with anti-leukemic activity. AS-99 TFA blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo.

HY-141429

AS-99 free base	Inhibitor
AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC₅₀= 0.79 µM, K_d= 0.89 µM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo.

HY-128717A

GSK3368715 dihydrochloride	Inhibitor	99.94%
GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC₅₀=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity.

HY-13500

GSK343	Inhibitor
GSK343 is a highly potent and selective EZH2 inhibitor with an IC₅₀ of 4 nM.

HY-101564

JNJ-64619178	Inhibitor	99.79%
JNJ-64619178 is a selective, orally active and pseudo-irreversible protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC₅₀ of 0.14 nM. JNJ-64619178 has potent activity In lung cancer.

HY-12727

EPZ015666	Inhibitor	99.83%
EPZ015666 (GSK3235025) is an orally available inhibitor of PRMT5 with an IC₅₀ of 22 nM.

HY-101117

EED226	Inhibitor	98.82%
EED226 is a polycomb repressive complex 2 (PRC2) inhibitor, which binds to the K27me3-pocket on embryonic ectoderm development (EED) and shows strong antitumor activity in xenograft mice model. EED226 is a potent, selective, and orally bioavailable EED inhibitor. EED226 inhibits PRC2 with an IC₅₀ of 23.4 nM when the H3K27me0 peptide is used as a substrate in the in vitro enzymatic assays.

HY-13980

UNC0642	Inhibitor
UNC0642 is a potent and selective lysine methyltransferases G9a and GLP inhibitor, with an IC₅₀ of <2.5 nM for G9a.

HY-15646

UNC1999	Inhibitor	99.85%
UNC1999 is a SAM-competitive, potent and selective inhibitor of EZH2/1 with IC₅₀s of <10 nM and 45 nM, repectively.

HY-19615

MS023	Inhibitor	99.12%
MS023 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.

HY-111109

EZM 2302	Inhibitor	99.49%
EZM 2302 is an inhibitor of coactivator-associated arginine methyltransferase 1 (CARM1) with an IC₅₀ of 6 nM.

HY-N2019

Chaetocin	Inhibitor	≥98.0%
Chaetocin is a specific inhibitor of the histone methyltransferase (HMT) SU(VAR)3-9 with an IC₅₀ of 0.6 μM for SU(VAR)3-9. It also inhibits thioredoxin reductase (TrxR) with an IC₅₀ of 4 μM.

HY-10587

BIX-01294	Inhibitor	≥98.0%
BIX-01294 is a reversible and highly selective G9a Histone Methyltransferase inhibitor, with an IC₅₀ of 2.7 μM in DELFIA assay. BIX-01294 specifically inhibits G9a (H3K9me2) and GLP enzyme (H3K9me3), with IC₅₀s of 1.7 μM and 38 μM, respectively. BIX-01294 inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 has antitumor activity in recurrent tumor cells.

HY-15273

UNC0638	Inhibitor	99.73%
UNC0638 selectively inhibits G9a and GLP histone methyltransferase activity with IC₅₀s of less than 15 nM and 19 nM, respectively. UNC0638 has anti-FMDV (foot-and-mouth disease virus) and anti-VSV (vesicular stomatitis virus) activities.

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