| 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.
|
Selective |
EZH1, IC50: 102.3 nM |
| 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 |
|
| 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. |
Pan |
EZH1, IC50: 6.1 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. |
Pan |
EZH1, IC50: 45 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. |
Pan |
EZH1, IC50: 52 nM |
| S7805 |
EPZ011989 |
EPZ011989 is a potent, selective, orally bioavailable EZH2 inhibitor with Ki of <3 nM. |
Pan |
EZH1, IC50: 103 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. |
Pan |
EZH1, IC50: 240 nM |
