Histone Methyltransferase

Signaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S7062 Pinometostat (EPZ5676) <1 mg/mL 100 mg/mL 92 mg/mL
S7004 EPZ005687 <1 mg/mL 2 mg/mL <1 mg/mL
S7164 GSK343 <1 mg/mL 1 mg/mL 4 mg/mL
S8006 BIX 01294 98 mg/mL 98 mg/mL 8 mg/mL
S7128 Tazemetostat (EPZ-6438) <1 mg/mL 5 mg/mL <1 mg/mL
S8624 JNJ-64619178 100 mg/mL
S8494 PF-06726304 <1 mg/mL 10 mg/mL 22 mg/mL
S8340 SGC2085 <1 mg/mL 62 mg/mL 62 mg/mL
S7983 A-196 <1 mg/mL 15 mg/mL 12 mg/mL
S7817 MI-503 <1 mg/mL 100 mg/mL 15 mg/mL
S7816 MI-463 <1 mg/mL 96 mg/mL 22 mg/mL
S7820 EPZ020411 2HCl 81 mg/mL 100 mg/mL 100 mg/mL
S8071 UNC0638 6 mg/mL 100 mg/mL 100 mg/mL
S8147 MS049 56 mg/mL 56 mg/mL 50 mg/mL
S8359 UNC3866 <1 mg/mL 100 mg/mL 46 mg/mL
S8353 CPI-1205 <1 mg/mL 100 mg/mL 100 mg/mL
S7833 OICR-9429 <1 mg/mL 38 mg/mL 14 mg/mL
S7120 3-deazaneplanocin A (DZNeP) HCl 52 mg/mL 52 mg/mL <1 mg/mL
S7165 UNC1999 <1 mg/mL 50 mg/mL 50 mg/mL
S7265 MM-102 100 mg/mL 100 mg/mL 100 mg/mL
S7079 SGC 0946 <1 mg/mL 100 mg/mL 100 mg/mL
S3147 Entacapone <1 mg/mL 61 mg/mL 2 mg/mL
S7570 UNC0379 <1 mg/mL 82 mg/mL
S7748 EPZ015666(GSK3235025) <1 mg/mL 60 mg/mL 48 mg/mL
S7294 PFI-2 HCl 4 mg/mL 99 mg/mL 25 mg/mL
S4589 Amodiaquine dihydrochloride dihydrate 29 mg/mL 92 mg/mL <1 mg/mL
S7832 SGC707 <1 mg/mL 59 mg/mL 59 mg/mL
S8112 MS023 <1 mg/mL 57 mg/mL 57 mg/mL
S8068 Chaetocin <1 mg/mL 100 mg/mL <1 mg/mL
S7619 MI-3 (Menin-MLL Inhibitor) <1 mg/mL 19 mg/mL 19 mg/mL
S7572 A-366 <1 mg/mL 65 mg/mL 65 mg/mL
S7591 BRD4770 <1 mg/mL 27 mg/mL <1 mg/mL
S7805 EPZ011989 <1 mg/mL <1 mg/mL 100 mg/mL
S7618 MI-2 (Menin-MLL Inhibitor) <1 mg/mL 75 mg/mL 75 mg/mL
S7575 LLY-507 <1 mg/mL 100 mg/mL 22 mg/mL
S8111 GSK591 <1 mg/mL 76 mg/mL 76 mg/mL
S8209 HLCL-61 HCL <1 mg/mL 76 mg/mL 76 mg/mL
S7611 EI1 <1 mg/mL 42 mg/mL <1 mg/mL
S7804 GSK503 <1 mg/mL 100 mg/mL 26 mg/mL
S7353 EPZ004777 <1 mg/mL 100 mg/mL 100 mg/mL
S7061 GSK126 <1 mg/mL 3 mg/mL <1 mg/mL
S7656 CPI-360 <1 mg/mL 20 mg/mL 18 mg/mL
S7616 CPI-169 <1 mg/mL 100 mg/mL 100 mg/mL
S7884 AMI-1 10 mg/mL 100 mg/mL <1 mg/mL
S7815 MI-136 <1 mg/mL 94 mg/mL 94 mg/mL
Catalog No. Information Product Use Citations Product Validations
S7062

Pinometostat (EPZ5676)

Pinometostat (EPZ5676) is an S-adenosyl methionine (SAM) competitive inhibitor of protein methyltransferase DOT1L with Ki of 80 pM in a cell-free assay, demonstrating >37,000-fold selectivity against all other PMTs tested, inhibits H3K79 methylation in tumor. Phase 1.

S7004

EPZ005687

EPZ005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM in a cell-free assay, 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.

S7164

GSK343

GSK343 is a potent and selective EZH2 inhibitor with IC50 of 4 nM in a cell-free assay, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other histone methyltransferases.

S8006

BIX 01294

BIX01294 is an inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM in a cell-free assay, reduces H3K9me2 of bulk histones, also weakly inhibits GLP (primarily H3K9me3), no significant activity observed at other histone methyltransferases.

S7128

Tazemetostat (EPZ-6438)

Tazemetostat (EPZ-6438) is a potent, and selective EZH2 inhibitor with Ki and IC50 of 2.5 nM and 11 nM in cell-free assays, exhibiting a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other HMTs.

S8624New

JNJ-64619178

JNJ-64619178 is a PRMT5 inhibitor with high selectivity and potency (subnanomolar range, PRMT5-MEP-50 IC50=0.14 nM) under different in vitro and cellular conditions, paired with favorable pharmacokinetics and safety properties.

S8494New

PF-06726304

PF-06726304 is a selective EZH2 inhibitor with Ki values of 0.7 nM and 3 nM for WT EZH2 and Y641N respectively; also inhibits H3K27me3 with the IC50 value of 15 nM.

S8340New

SGC2085

SGC2085 is a potent and selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) inhibitor with an IC50 value of 50 nM and >100-fold selective over other PRMTs.

S7983New

A-196

A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC50 values of 0.025 and 0.144 μM, respectively; more than 100-fold selective over other histone methyltransferases and non-epigenetic targets.

S7817New

MI-503

MI-503 is a potent and selective Menin-MLL inhibitor with IC50 of 14.7 nM. It shows pronounced growth suppressive activity in a panel of human MLL leukemia cell lines(GI50 at 250 nM-570 nM range), but only a minimal effect in human leukemia cell lines without MLL translocations.

S7816New

MI-463

MI-463 is a potent inhibitor of Menin-MLL interaction with an IC50 value of 15.3 nM.

S7820New

EPZ020411 2HCl

EPZ020411 is a potent and selective small molecule PRMT6 inhibitor with an IC50 of 10 nM.

S8071New

UNC0638

UNC0638 is a potent, selective and cell-penetrant chemical probe for G9a and GLP with IC50 of <15 nM and 19 nM, respectively, shows selectivity over a wide range of epigenetic and non-epigenetic targets.

S8147New

MS049

MS049 is a potent and selective inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively.

S8359New

UNC3866

UNC3866 is a potent antagonist of the methyllysine (Kme) reading function of the Polycomb CBX and CDY families of chromodomains. UNC3866 binds the chromodomains of CBX4 and CBX7 most potently, with a K(d) of ∼100 nM for each, and is 6- to 18-fold selective as compared to seven other CBX and CDY chromodomains.

S8353New

CPI-1205

CPI-1205 is an orally available selective inhibitor of the histone lysine methyltransferase EZH2, with potential antineoplastic activity.

S7833New

OICR-9429

OICR-9429 is a potent antagonist of the interaction of WDR5 with peptide regions of MLL and Histone 3 and reduces viability of acute myeloid leukemia cells in vitro.

S7120

3-deazaneplanocin A (DZNeP) HCl

3-deazaneplanocin A (DZNeP)HCl, an analog of adenosine, is a competitive inhibitor of S-adenosylhomocysteine hydrolase with Ki of 50 pM in a cell-free assay.

S7165

UNC1999

UNC1999 is a potent, orally bioavailable and selective inhibitor of EZH2 and EZH1 with IC50 of 2 nM and 45 nM in cell-free assays, respectively, showing >1000-fold selectivity over a broad range of epigenetic and non-epigenetic targets.

S7265

MM-102

MM-102 is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM in a cell-free assay.

S7079

SGC 0946

SGC 0946 is a highly potent and selective DOT1L methyltransferase inhibitor with IC50 of 0.3 nM in a cell-free assay, is inactive against a panel of 12 PMTs and DNMT1.

S3147

Entacapone

Entacapone inhibits catechol-O-methyltransferase(COMT) with IC50 of 151 nM.

S7570

UNC0379

UNC0379 is a selective, substrate competitive inhibitor of N-lysine methyltransferase SETD8 with IC50 of 7.9 μM, high selectivity over 15 other methyltransferases.

S7748

EPZ015666(GSK3235025)

EPZ015666(GSK3235025) is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs.

S7294

PFI-2 HCl

PFI-2 is a potent, selective, and cell-active lysine methyltransferase SETD7 inhibitor with Ki (app) and IC50 of 0.33 nM and 2 nM, 1000-fold selectivity over other methyltransferases and other non-epigenetic targets.

S4589

Amodiaquine dihydrochloride dihydrate

Amodiaquine is a potent, non-competitive inhibitor of histamine N-methyl transferase in human erythrocytes, also used as an antimalarial and anti-inflammatory agent.

S7832

SGC707

SGC707 is a potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3) with IC50 and Kd of 31 nM and 53 nM, respectively.

S8112

MS023

MS023 is a potent, selective, and cell-active Type I PRMT inhibitor with IC50 of 30 nM, 119 nM, 83 nM, 4 nM, and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6 and PRMT8, respectively.

S8068

Chaetocin

Chaetocin, a natural product from Chaetomium species, is a histone methyltransferase inhibitor with IC50 of 0.8 μM, 2.5 μM and 3 μM for dSU(VAR)3-9, mouse G9a and Neurospora crassa DIM5, respectively.

S7619

MI-3 (Menin-MLL Inhibitor)

MI-3 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 648 nM.

S7572

A-366

A-366 is a potent and selective G9a/GLP histone lysine methyltransferase inhibitor with IC50 of 3.3nM, exhibiting >1000-fold selectivity for G9a/GLP over 21 other methyltransferases.

S7591

BRD4770

BRD4770 is a histone methyltransferase G9a inhibitor with IC50 of 6.3 μM, and induces cell senescence.

S7805

EPZ011989

EPZ011989 is a potent, selective, orally bioavailable EZH2 inhibitor with Ki of <3 nM.

S7618

MI-2 (Menin-MLL Inhibitor)

MI-2 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 446 nM.

S7575

LLY-507

LLY-507 is a cell-active, potent, and selective inhibitor of protein-lysine Methyltransferase SMYD2.

S8111

GSK591

GSK591 (EPZ015866,GSK3203591) is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 11 nM.

S8209

HLCL-61 HCL

HLCL-61 hydrochloride is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukemia.

S7611

EI1

EI1 is a potent and selective EZH2 inhibitor with IC50 of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively.

S7804

GSK503

GSK503 is a potent and specific EZH2 methyltransferase inhibitor.

S7353

EPZ004777

EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM in a cell-free assay and demonstrates >1,200-fold selectivity for DOT1L over all other tested PMTs.

S7061

GSK126

GSK126 is a potent, highly selective EZH2 methyltransferase inhibitor with IC50 of 9.9 nM, >1000-fold selective for EZH2 over 20 other human methyltransferases.

S7656

CPI-360

CPI-360 is a potent, selective,and SAM-competitive EZH1 inhibitor with IC50 of 102.3 nM, >100-fold selectivity over other methyltransferases.

S7616

CPI-169

CPI-169 is a potent, and selective EZH2 inhibitor with IC50 of 0.24 nM, 0.51 nM, and 6.1 nM for EZH2 WT, EZH2 Y641N, and EZH1, respectively.

S7884

AMI-1

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.

S7815

MI-136

MI-136 can specifically inhibit the menin-MLL interaction. It inhibits DHT-induced expression of androgen receptor (AR) target genes.