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. |
-
Cancer Cell, 2021, 39(3):407-422.e13
-
Cancer Biol Ther, 2021, 22(4):333-344
-
Nat Commun, 2020, 11(1):604
|
|
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. |
-
Nat Cell Biol, 2022, 24(3):384-399
-
Nat Commun, 2022, 13(1):12
-
Cancer Metab, 2022, 10(1):4
|
|
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. |
-
Nat Cell Biol, 2022, 24(3):384-399
-
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
-
Nat Commun, 2022, 13(1):12
|
|
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. |
-
Hepatology, 2022, 10.1002/hep.32443
-
Theranostics, 2022, 12(5):2063-2079
-
J Immunol, 2022, 208(2):347-357
|
|
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. |
-
Pharmacol Res, 2022, 177:106122
-
J Immunol, 2022, 208(2):347-357
-
Hepatology, 2021, 10.1002/hep.32245
|
|
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.
|
-
Cancer Res, 2018, 78(20):5731-5740
-
Mol Cancer, 2017, 10.1186/s12943-016-0575-6
-
Virology, 2017, 506:34-44
|
|
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. |
-
Cell Chem Biol, 2021, S2451-9456(21)00213-0
-
Cancer Sci, 2020, 112(1):133-143
-
J Clin Invest, 2020, 134217
|
|
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.
|
-
Cancer Res, 2018, 78(20):5731-5740
|
|
S7804 |
GSK503
|
GSK503 is a potent and specific EZH2 methyltransferase inhibitor.
|
-
Cancer Cell, 2019, 36(4):385-401
-
Cancer Res, 2018, 78(20):5731-5740
-
J Pathol, 2018, 245(4):433-444
|
|
S7805 |
EPZ011989
|
EPZ011989 is a potent, selective, orally bioavailable EZH2 inhibitor with Ki of <3 nM. |
-
Neuron, 2022, S0896-6273(21)01089-8
-
Mol Neurobiol, 2022, 10.1007/s12035-021-02602-8
-
Mol Cancer Ther, 2021, 20(3):541-552
|
|
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. |
-
Nat Commun, 2021, 12(1):6276
-
J Immunother Cancer, 2021, 9(5)e001335
-
Cancer Discov, 2021, candisc.0913.2020
|
|
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.
|
-
Elife, 2021, 10e65654
|
|
S8607 |
JQ-EZ-05 (JQEZ5)
|
JQ-EZ-05 (JQEZ5) is a specific and reversible EZH1/2 inhibitor. |
-
Nat Chem Biol, 2019, 15(4):391-400
|
|
S8702 |
EBI-2511
|
EBI-2511 is a highly potent and orally active EZH2 inhibitor with an IC50 of 4 nM for EZH2(A667G). |
|
|
S8926 |
Valemetostat (DS-3201)
|
Valemetostat (DS-3201, DS-3201b) is a selective EZH1/2 dual inhibitor. |
|
|
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. |
-
Oncotarget, 2021, 12(6):549-561
-
Cancer Lett, 2020, 469:277-286
|
|
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. |
- Cancer Cell, 2021, 39(3):407-422.e13
- Cancer Biol Ther, 2021, 22(4):333-344
- Nat Commun, 2020, 11(1):604
|
|
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. |
- Nat Cell Biol, 2022, 24(3):384-399
- Nat Commun, 2022, 13(1):12
- Cancer Metab, 2022, 10(1):4
|
|
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. |
- Nat Cell Biol, 2022, 24(3):384-399
- Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
- Nat Commun, 2022, 13(1):12
|
|
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. |
- Hepatology, 2022, 10.1002/hep.32443
- Theranostics, 2022, 12(5):2063-2079
- J Immunol, 2022, 208(2):347-357
|
|
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. |
- Pharmacol Res, 2022, 177:106122
- J Immunol, 2022, 208(2):347-357
- Hepatology, 2021, 10.1002/hep.32245
|
|
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.
|
- Cancer Res, 2018, 78(20):5731-5740
- Mol Cancer, 2017, 10.1186/s12943-016-0575-6
- Virology, 2017, 506:34-44
|
|
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. |
- Cell Chem Biol, 2021, S2451-9456(21)00213-0
- Cancer Sci, 2020, 112(1):133-143
- J Clin Invest, 2020, 134217
|
|
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.
|
- Cancer Res, 2018, 78(20):5731-5740
|
|
S7804 |
GSK503
|
GSK503 is a potent and specific EZH2 methyltransferase inhibitor.
|
- Cancer Cell, 2019, 36(4):385-401
- Cancer Res, 2018, 78(20):5731-5740
- J Pathol, 2018, 245(4):433-444
|
|
S7805 |
EPZ011989
|
EPZ011989 is a potent, selective, orally bioavailable EZH2 inhibitor with Ki of <3 nM. |
- Neuron, 2022, S0896-6273(21)01089-8
- Mol Neurobiol, 2022, 10.1007/s12035-021-02602-8
- Mol Cancer Ther, 2021, 20(3):541-552
|
|
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. |
- Nat Commun, 2021, 12(1):6276
- J Immunother Cancer, 2021, 9(5)e001335
- Cancer Discov, 2021, candisc.0913.2020
|
|
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.
|
- Elife, 2021, 10e65654
|
|
S8607 |
JQ-EZ-05 (JQEZ5)
|
JQ-EZ-05 (JQEZ5) is a specific and reversible EZH1/2 inhibitor. |
- Nat Chem Biol, 2019, 15(4):391-400
|
|
S8702 |
EBI-2511
|
EBI-2511 is a highly potent and orally active EZH2 inhibitor with an IC50 of 4 nM for EZH2(A667G). |
|
|
S8926 |
Valemetostat (DS-3201)
|
Valemetostat (DS-3201, DS-3201b) is a selective EZH1/2 dual inhibitor. |
|
|
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. |
- Oncotarget, 2021, 12(6):549-561
- Cancer Lett, 2020, 469:277-286
|
|