Histone Methyltransferase

Sigaling 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
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 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 15 mg/mL
S7575 LLY-507 <1 mg/mL 100 mg/mL 22 mg/mL
S4589 Amodiaquine dihydrochloride dihydrate 29 mg/mL 92 mg/mL <1 mg/mL
S7572 A-366 <1 mg/mL 65 mg/mL 65 mg/mL
S7815 MI-136 <1 mg/mL 94 mg/mL 94 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
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 4 mg/mL 99 mg/mL 66 mg/mL
S7610 UNC0631 <1 mg/mL 100 mg/mL 5 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
S7591 BRD4770 <1 mg/mL 27 mg/mL <1 mg/mL
S7618 MI-2 (Menin-MLL Inhibitor) <1 mg/mL 75 mg/mL 75 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
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.

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

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.

S7575New

LLY-507

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

S4589New

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.

S7572New

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.

S7815New

MI-136

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

S8111New

GSK591

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

S8209New

HLCL-61 HCL

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

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

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.

S7610

UNC0631

UNC0631 is a potent histone methyltransferase G9a inhibitor with IC50 of 4 nM.

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.

S7591

BRD4770

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

S7618

MI-2 (Menin-MLL Inhibitor)

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

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.

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.

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.

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

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.

S7575New

LLY-507

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

S4589New

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.

S7572New

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.

S7815New

MI-136

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

S8111New

GSK591

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

S8209New

HLCL-61 HCL

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

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

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.

S7610

UNC0631

UNC0631 is a potent histone methyltransferase G9a inhibitor with IC50 of 4 nM.

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.

S7591

BRD4770

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

S7618

MI-2 (Menin-MLL Inhibitor)

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

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.

Catalog No. Information Product Use Citations Product Validations
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.