• EZH2
  • EZH1

EZH2 Selective Inhibitors

Catalog No. Product Name Information Selective / Pan IC50 / Ki
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. Selective EZH2 Y641N, IC50: 0.51 nM; EZH2 WT, IC50: 0.24 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. Selective EZH2 Y641N, Ki: 3 nM; Ezh2 (wild-type), Ki: 0.7 nM
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. UNC1999 is a potent autophagy inducer. UNC1999 specifically suppresses H3K27me3/2 and induces a range of anti-leukemia effects including anti-proliferation, differentiation, and apoptosis. Selective EZH2, IC50: 2 nM
S8353 Lirametostat (CPI-1205) Lirametostat (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. Selective EZH2, IC50: 2 nM
S7128 Tazemetostat (EPZ-6438) Tazemetostat (EPZ-6438, E7438) 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. Selective EZH2, Ki: 2.5 nM
S7805 EPZ011989 EPZ011989 is a potent, selective, orally bioavailable EZH2 inhibitor with Ki of <3 nM. Selective EZH2, Ki: <3 nM
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. GSK343 induces autophagy. Selective EZH2, IC50: 4 nM
S8702 EBI-2511 EBI-2511 is a highly potent and orally active EZH2 inhibitor with an IC50 of 4 nM for EZH2(A667G). Selective EZH2(A667G), IC50: 4 nM
S7804 GSK503 GSK503 is a potent and specific EZH2 methyltransferase inhibitor. Selective EZH2, IC50: 8 nM
S7061 GSK126 GSK126 (GSK2816126A, GSK2816126) is a potent, highly selective EZH2 methyltransferase inhibitor with IC50 of 9.9 nM, >1000-fold selective for EZH2 over 20 other human methyltransferases. Selective EZH2, IC50: 9.9 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. Selective EZH2 (Y641F), IC50: 13 nM; Ezh2 (wild-type), IC50: 15 nM
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. Selective EZH2, Ki: 24 nM
S9031 Gambogenic acid Gambogenic Acid, identified from Gamboge, is an inhibitor of the FGFR signaling pathway in erlotinib-resistant non-small-cell lung cancer (NSCLC) and exhibits anti-tumor effects. Gambogenic acid acts is also an effective inhibitor of EZH2 that specifically and covalently binds to Cys668 within the EZH2-SET domain, and triggers EZH2 ubiquitination. Selective
S8607 JQ-EZ-05 (JQEZ5) JQ-EZ-05 (JQEZ5) is a specific and reversible EZH1/2 inhibitor. Pan
S8926 Valemetostat (DS-3201) Valemetostat (DS-3201, DS-3201b) is a selective EZH1/2 dual inhibitor. Pan