Histone Methyltransferase

Histone Methyltransferase Related Products (123):

By Effects:	Inhibitors (115) Antagonists (8)

Cat. No.	Product Name	Effect	Purity

HY-13470

GSK126 Inhibitor 99.98%

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

GSK126	Inhibitor	99.98%
GSK126 (GSK2816126A) is a potent, highly selective inhibitor of EZH2 methyltransferase with an IC₅₀ of 9.9 nM.

HY-13803

Tazemetostat	Inhibitor	99.76%
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-15593

Pinometostat Inhibitor 99.92%

Pinometostat (EPZ-5676) is a potent DOT1L histone methyltransferase inhibitor with a K_i of 80 pM.
HY-101563

GSK3326595 Inhibitor 99.55%

GSK3326595 is a potent, selective, reversible inhibitor of protein arginine methyltransferase 5 (PRMT5) with an IC₅₀ of 6.2 nM.
HY-12186

3-Deazaneplanocin A hydrochloride Inhibitor 99.76%

3-Deazaneplanocin A hydrochloride is a potent histone methyltransferase EZH2 inhibitor.

Pinometostat	Inhibitor	99.92%
Pinometostat (EPZ-5676) is a potent DOT1L histone methyltransferase inhibitor with a K_i of 80 pM.

GSK3326595	Inhibitor	99.55%
GSK3326595 is a potent, selective, reversible inhibitor of protein arginine methyltransferase 5 (PRMT5) with an IC₅₀ of 6.2 nM.

3-Deazaneplanocin A hydrochloride	Inhibitor	99.76%
3-Deazaneplanocin A hydrochloride is a potent histone methyltransferase EZH2 inhibitor.

HY-N5024

Gambogenic acid	Inhibitor	99.91%
Gambogenic acid is an active ingredient in gamboge, with anticancer activity. Gambogenic acid acts as an effective inhibitor of EZH2, specifically and covalently binds to Cys668 within the EZH2-SET domain, and induces EZH2 ubiquitination.

HY-114208A

BI-9321 trihydrochloride	Antagonist
BI-9321 trihydrochloride is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a K_d value of 166 nM. BI-9321 trihydrochloride is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 trihydrochloride specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC₅₀ of 1.2 μM in U2OS cells.

HY-101925

CM-272	Inhibitor
CM-272 is a first-in-class, potent, selective, substrate-competitive and reversible dual G9a/DNA methyltransferases (DNMTs) inhibitor. CM-272 inhibits G9a, DNMT1, DNMT3A, DNMT3B and GLP with IC₅₀s of 8 nM, 382 nM, 85 nM, 1200 nM and 2 nM, respectively. CM-272 inhibits cell proliferation and promotes apoptosis, inducing interferon-stimulated genes and immunogenic cell death. Anti-tumour Activity.

HY-13500

GSK343 Inhibitor 99.45%

GSK343 is a highly potent and selective EZH2 inhibitor with an IC₅₀ of 4 nM.
HY-13980

UNC0642 Inhibitor 99.81%

UNC0642 is a potent and selective lysine methyltransferases G9a and GLP inhibitor, with an IC₅₀ of <2.5 nM for G9a.
HY-10587

BIX-01294 Inhibitor 98.61%

BIX-01294 is an inhibitor of G9a Histone Methyltransferase with an IC₅₀ of 1.9 μM.

GSK343	Inhibitor	99.45%
GSK343 is a highly potent and selective EZH2 inhibitor with an IC₅₀ of 4 nM.

UNC0642	Inhibitor	99.81%
UNC0642 is a potent and selective lysine methyltransferases G9a and GLP inhibitor, with an IC₅₀ of <2.5 nM for G9a.

BIX-01294	Inhibitor	98.61%
BIX-01294 is an inhibitor of G9a Histone Methyltransferase with an IC₅₀ of 1.9 μM.

HY-19615

MS023	Inhibitor	99.50%
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-101564

JNJ-64619178 Inhibitor 99.02%

JNJ-64619178 is a selective, orally active and pseudo-irreversible 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.

JNJ-64619178	Inhibitor	99.02%
JNJ-64619178 is a selective, orally active and pseudo-irreversible PRMT5 inhibitor with an IC₅₀ of 0.14 nM. JNJ-64619178 has potent activity In lung cancer.

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

HY-N2019

Chaetocin	Inhibitor	98.06%
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-101117

EED226	Inhibitor	98.70%
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-15650

SGC0946 Inhibitor 99.68%

SGC0946 is a highly potent and selective DOT1L methyltransferase inhibitor with IC50 of 0.3 nM; selectively kill mixed lineage leukaemia cells.
HY-15227

EPZ004777 Inhibitor 99.46%

EPZ004777 is a potent, selective DOT1L inhibitor with an IC₅₀ of 0.4 nM.
HY-15646

UNC1999 Inhibitor 99.47%

UNC1999 is a SAM-competitive, potent and selective inhibitor of EZH2/1 with IC₅₀s of <10 nM and 45 nM, repectively.
HY-16993

OICR-9429 Antagonist 99.94%

OICR-9429 is a novel small-molecule antagonist of the Wdr5-MLL interaction with IC50 of 5 uM.

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