Signaling Pathway

Histone Methyltransferase

Histone Methyltransferase

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Histone Methyltransferase Inhibitors & Modulators (56)

Product Name Catalog No. Brief Description
3-Deazaneplanocin A

HY-10442

3-Deazaneplanocin A (DZNep) is an attractive epigenetic anticancer agent through the inhibition of the cellular enhancer of zeste homolog 2 (EZH2) protein.

3-Deazaneplanocin A hydrochloride

HY-12186

3-Deazaneplanocin A hydrochloride(DZNep hydrochloride) is an attractive epigenetic anticancer agent through the inhibition of the cellular enhancer of zeste homolog 2 (EZH2) protein.

A-366

HY-12583

A-366 is a peptide-competitive inhibitor of G9a/GLP with an enzymatic IC50 of ~3 nM and >100-fold selectivity over other methyltransferases and other non-epigenetic targets.

AMI-1

HY-18962

AMI-1 is a potent, cell-permeable compound which inhibits protein arginine N-methyltransferases (PRMTs), including human PRMT1 (IC50 = 8.8μM) and yeast-Hmt1p (IC50 = 3.0μM), by blocking peptide-substrate binding.

Amodiaquin dihydrochloride dihydrate

HY-B1322

Amodiaquine dihydrochloride dihydrate is a histamine N-methyltransferase inhibitor, used as an antimalarial and anti-inflammatory agent.

AZ505

HY-15226

AZ505 is a potent and highly selective inhibitor of the oncogenic protein SMYD2(IC50=0.12 uM) with potential anticancer activity, >600 fold than SMYD3(IC50>83.3 uM); DOT1L(IC50>83.3 uM);EZH2(IC50>83.3 uM).

AZ505 ditrifluoroacetate

HY-15226A

AZ505 ditrifluoroacetate is a potent and highly selective inhibitor of the oncogenic protein SMYD2(IC50=0.12 uM) with potential anticancer activity, >600 fold than SMYD3(IC50>83.3 uM); DOT1L(IC50>83.3 uM);EZH2(IC50>83.3 uM).

BIX-01294

HY-10587

BIX01294 is an inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM.

BRD4770

HY-16705

BRD4770 is a novel G9a(EHMT2) inhibitor with EC50 of 5 uM (trimethylated H3K9 in PANC-1 cell).

BRD9539

HY-15647

BRD9539 inhibits G9a activity with an IC50 of 6.3 μM, inhibits PRC2 activity with a similar IC50.

C-7280948

HY-15890

C-7280948 is a PRMT1 inhibitor.

CARM1-IN-1

HY-12759

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).

CARM1-IN-1 hydrochloride

HY-12759A

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).

EI1

HY-15573

EI1 is a potent and selective small molecule inhibitor of EZH2 with IC50 values of 15 nM and 13 nM for wild type EZH2 and EZH2 Y641F mutant, respectively.

EPZ-5676

HY-15593

EPZ-5676 is a potent and selective aminonucleoside inhibitor of DOT1L histone methyltransferase with Ki of 80 pM; demonstrating >37,000-fold selectivity against all other PMTs tested, inhibits H3K79 methylation in tumor.

EPZ-6438

HY-13803

EPZ-6438 is a potent, selective, and orally bioavailable small-molecule inhibitor of EZH2 enzymatic activity with Ki value of 2.5±0.5 nM.

EPZ004777

HY-15227

EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.

EPZ004777 hydrochloride

HY-15227A

EPZ004777 hydrochloride is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.

EPZ005687

HY-15555

EPZ-005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM, 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.

EPZ011989

HY-16986

EPZ011989 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.