EZH1/2

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Catalog No. Product Name 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.
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
Tags: EZH1/2 inhibitors | EZH1/2 modulators | EZH1/2 chemical | EZH1/2 Inhibition