EZH1/2

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S7004 EPZ005687 <1 mg/mL 2 mg/mL <1 mg/mL
S7164 GSK343 <1 mg/mL 1 mg/mL 4 mg/mL
S7128 Tazemetostat (EPZ-6438) <1 mg/mL 5 mg/mL <1 mg/mL
S7165 UNC1999 <1 mg/mL 20 mg/mL 50 mg/mL
S8353 CPI-1205 <1 mg/mL 100 mg/mL 100 mg/mL
S7805 EPZ011989 <1 mg/mL <1 mg/mL 100 mg/mL
S8494 PF-06726304 <1 mg/mL 10 mg/mL 22 mg/mL
S7611 EI1 <1 mg/mL 42 mg/mL <1 mg/mL
S7804 GSK503 <1 mg/mL 100 mg/mL 26 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
Catalog No. Information Product Use Citations Product Validations
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.

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.

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.

S8607New

JQ-EZ-05 (JQEZ5)

JQ-EZ-05 is a specific and reversible EZH1/2 inhibitor.

S8353

CPI-1205

CPI-1205 is an orally available selective inhibitor of the histone lysine methyltransferase EZH2 with IC50 values of 2 nM and 52 nM for EZH2 and EZH1 respectively. It has potential antineoplastic activity.

S7805

EPZ011989

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

S8494

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.

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.

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.

Tags: EZH1/2 inhibitors | EZH1/2 modulators | EZH1/2 chemical | EZH1/2 Inhibition