| 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 WT, IC50: 0.24 nM; EZH2 Y641N, IC50: 0.51 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 (wild-type), Ki: 0.7 nM; EZH2 Y641N, Ki: 3 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 |
| 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 |
| 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 (wild-type), IC50: 15 nM; EZH2 (Y641F), IC50: 13 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 |
|
| S8926 |
Valemetostat (DS-3201) |
Valemetostat (DS-3201, DS-3201b) is a selective EZH1/2 dual inhibitor. |
Pan |
|
| S8607 |
JQ-EZ-05 (JQEZ5) |
JQ-EZ-05 (JQEZ5) is a specific and reversible EZH1/2 inhibitor. |
Pan |
|
