Histone Methyltransferase

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Histone Methyltransferase Inhibitors (25)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
S7062 EPZ5676 EPZ-5676 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.
  • Cell Rep, 2014, 9(3):1163-70
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.
  • Oncogene, 2015, 10.1038/onc.2015.38
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.
  • Oncogene, 2015, 10.1038/onc.2015.38
  • Oncotarget, 2015, 6(32):32410-25
  • Clin Exp Pharmacol Physiol, 2015, 10.1111/1440-1681.12382
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) 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.
  • Klin Padiatr, 2016, 228(3):113-117
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.
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.
S7804 GSK503 GSK503 is a potent and specific EZH2 methyltransferase inhibitor.
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.
  • J Infect Dis, 2016, 10.1093/infdis/jiw226
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.
  • Oncogene, 2015, 10.1038/onc.2015.38
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.
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.
S7748 EPZ015666 EPZ015666 is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other 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.
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.
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.
  • Oncotarget, 2015, 6(32):32410-25
S7591 BRD4770 BRD4770 is a histone methyltransferase G9a inhibitor with IC50 of 6.3 μM, and induces cell senescence.
S7610 UNC0631 UNC0631 is a potent histone methyltransferase G9a inhibitor with IC50 of 4 nM.
S7618 MI-2 (Menin-MLL Inhibitor) MI-2 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 446 nM.
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.
S7619 MI-3 (Menin-MLL Inhibitor) MI-3 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 648 nM.
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.
S7265 MM-102 MM-102 is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM in a cell-free assay.
S7353 EPZ004777 EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM in a cell-free assay.
  • Reprod Fertil Dev, 2014, 27(1):106
S3147 Entacapone Entacapone inhibits catechol-O-methyltransferase(COMT) with IC50 of 151 nM.

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S7062 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 4 mg/mL <1 mg/mL
S7832 SGC707 <1 mg/mL 59 mg/mL 59 mg/mL
S7656 CPI-360 <1 mg/mL 20 mg/mL 18 mg/mL
S7804 GSK503 <1 mg/mL 100 mg/mL 26 mg/mL
S7120 3-deazaneplanocin A (DZNeP) HCl 52 mg/mL 52 mg/mL <1 mg/mL
S7165 UNC1999 <1 mg/mL 100 mg/mL 100 mg/mL
S7884 AMI-1 10 mg/mL 100 mg/mL <1 mg/mL
S7616 CPI-169 <1 mg/mL 100 mg/mL 100 mg/mL
S7748 EPZ015666 <1 mg/mL 60 mg/mL 48 mg/mL
S7061 GSK126 <1 mg/mL 3 mg/mL <1 mg/mL
S7570 UNC0379 <1 mg/mL 82 mg/mL
S7611 EI1 <1 mg/mL 42 mg/mL <1 mg/mL
S7591 BRD4770 <1 mg/mL 27 mg/mL <1 mg/mL
S7610 UNC0631 <1 mg/mL 100 mg/mL 5 mg/mL
S7618 MI-2 (Menin-MLL Inhibitor) <1 mg/mL 75 mg/mL 75 mg/mL
S7294 PFI-2 4 mg/mL 99 mg/mL 66 mg/mL
S7619 MI-3 (Menin-MLL Inhibitor) <1 mg/mL 19 mg/mL 19 mg/mL
S7079 SGC 0946 <1 mg/mL 100 mg/mL 100 mg/mL
S7265 MM-102 100 mg/mL 100 mg/mL 100 mg/mL
S7353 EPZ004777 <1 mg/mL 100 mg/mL 100 mg/mL
S3147 Entacapone <1 mg/mL 61 mg/mL 2 mg/mL
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