S7061 |
GSK126
|
GSK126 (GSK2816126A、GSK2816126) は強力で選択性の高い EZH2 メチルトランスフェラーゼ (methyltransferase) 阻害剤(IC50=9.9 nM)であり、EZH2 に対して 20 種類以上の他のヒトメチルトランスフェラーゼよりも 1000 倍以上の選択性を持ちます。 |
-
Signal Transduct Target Ther, 2024, 9(1):2
-
Cell, 2023, 186(13):2765-2782.e28
-
Mol Cancer, 2023, 22(1):85
|
|
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. |
-
Signal Transduct Target Ther, 2024, 9(1):2
-
Nat Commun, 2024, 15(1):1367
-
Sci Rep, 2024, 14(1):4303
|
|
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. |
-
J Immunother Cancer, 2023, 11(11)e007736
-
Clin Transl Med, 2023, 13(12):e1502
-
J Neuroinflammation, 2023, 20(1):168
|
|
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. |
-
Acta Pharm Sin B, 2023, 13(6):2601-2612
-
J Exp Clin Cancer Res, 2023, 42(1):320
-
Pharmacol Res, 2022, 177:106122
|
|
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. |
-
J Exp Clin Cancer Res, 2023, 42(1):320
-
BMC Med, 2022, 20(1):189
-
Cancers (Basel), 2022, 15(1)208
|
|
S7805 |
EPZ011989
|
EPZ011989 is a potent, selective, orally bioavailable EZH2 inhibitor with Ki of <3 nM. |
-
Cancers (Basel), 2024, 16(3):569.
-
Cancers (Basel), 2024, 16(3)569
-
Nat Cell Biol, 2023, 25(2):258-272
|
|
S8353 |
Lirametostat (CPI-1205)
|
Lirametostat (CPI-1205) is an orally available selective inhibitor of the histone lysine methyltransferase EZH2, with potential antineoplastic activity. |
-
JCI Insight, 2022, e155899
-
Cancer Discov, 2021, candisc.0913.2020
-
Nat Commun, 2021, 12(1):6276
|
|
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. |
-
J Exp Clin Cancer Res, 2023, 42(1):96
-
Nat Commun, 2022, 13(1):6226
-
Nat Commun, 2022, 13(1):6226
|
|
S7804 |
GSK503
|
GSK503 is a potent and specific EZH2 methyltransferase inhibitor.
|
-
Int J Mol Sci, 2023, 24(10)8603
-
Cancer Res, 2022, CAN-22-0736
-
Front Genet, 2022, 13:1013475
|
|
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
|
|
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. |
-
Chem Biol Interact, 2023, 382:110602
-
Oncotarget, 2021, 12(6):549-561
-
Cancer Lett, 2020, 469:277-286
|
|
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.
|
-
Nat Commun, 2023, 10.1038/s41467-023-42930-y
-
Elife, 2021, 10e65654
|
|
S8926 |
Valemetostat (DS-3201)
|
Valemetostat (DS-3201, DS-3201b) is a selective EZH1/2 dual inhibitor. |
-
Nucleic Acids Res, 2023, gkad387
-
J Physiol, 2022, 600(14):3331-3353
|
|
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.
|
-
Mol Ther Oncolytics, 2022, 27:14-25
-
Cancer Res, 2018, 78(20):5731-5740
|
|
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). |
|
|
E1497New |
Tulmimetostat
|
Tulmimetostat (CPI-0209) is an orally bioavailable and selective inhibitor of EZH2 that has therapeutic potential for androgen receptor-dependent prostate cancer. |
|
|
S7061 |
GSK126
|
GSK126 (GSK2816126A、GSK2816126) は強力で選択性の高い EZH2 メチルトランスフェラーゼ (methyltransferase) 阻害剤(IC50=9.9 nM)であり、EZH2 に対して 20 種類以上の他のヒトメチルトランスフェラーゼよりも 1000 倍以上の選択性を持ちます。 |
- Signal Transduct Target Ther, 2024, 9(1):2
- Cell, 2023, 186(13):2765-2782.e28
- Mol Cancer, 2023, 22(1):85
|
|
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. |
- Signal Transduct Target Ther, 2024, 9(1):2
- Nat Commun, 2024, 15(1):1367
- Sci Rep, 2024, 14(1):4303
|
|
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. |
- J Immunother Cancer, 2023, 11(11)e007736
- Clin Transl Med, 2023, 13(12):e1502
- J Neuroinflammation, 2023, 20(1):168
|
|
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. |
- Acta Pharm Sin B, 2023, 13(6):2601-2612
- J Exp Clin Cancer Res, 2023, 42(1):320
- Pharmacol Res, 2022, 177:106122
|
|
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. |
- J Exp Clin Cancer Res, 2023, 42(1):320
- BMC Med, 2022, 20(1):189
- Cancers (Basel), 2022, 15(1)208
|
|
S7805 |
EPZ011989
|
EPZ011989 is a potent, selective, orally bioavailable EZH2 inhibitor with Ki of <3 nM. |
- Cancers (Basel), 2024, 16(3):569.
- Cancers (Basel), 2024, 16(3)569
- Nat Cell Biol, 2023, 25(2):258-272
|
|
S8353 |
Lirametostat (CPI-1205)
|
Lirametostat (CPI-1205) is an orally available selective inhibitor of the histone lysine methyltransferase EZH2, with potential antineoplastic activity. |
- JCI Insight, 2022, e155899
- Cancer Discov, 2021, candisc.0913.2020
- Nat Commun, 2021, 12(1):6276
|
|
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. |
- J Exp Clin Cancer Res, 2023, 42(1):96
- Nat Commun, 2022, 13(1):6226
- Nat Commun, 2022, 13(1):6226
|
|
S7804 |
GSK503
|
GSK503 is a potent and specific EZH2 methyltransferase inhibitor.
|
- Int J Mol Sci, 2023, 24(10)8603
- Cancer Res, 2022, CAN-22-0736
- Front Genet, 2022, 13:1013475
|
|
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
|
|
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. |
- Chem Biol Interact, 2023, 382:110602
- Oncotarget, 2021, 12(6):549-561
- Cancer Lett, 2020, 469:277-286
|
|
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.
|
- Nat Commun, 2023, 10.1038/s41467-023-42930-y
- Elife, 2021, 10e65654
|
|
S8926 |
Valemetostat (DS-3201)
|
Valemetostat (DS-3201, DS-3201b) is a selective EZH1/2 dual inhibitor. |
- Nucleic Acids Res, 2023, gkad387
- J Physiol, 2022, 600(14):3331-3353
|
|
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.
|
- Mol Ther Oncolytics, 2022, 27:14-25
- Cancer Res, 2018, 78(20):5731-5740
|
|
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). |
|
|
E1497New |
Tulmimetostat
|
Tulmimetostat (CPI-0209) is an orally bioavailable and selective inhibitor of EZH2 that has therapeutic potential for androgen receptor-dependent prostate cancer. |
|
|