EZH1/2

亜型選択性的な製品

EZH1/2製品

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  • EZH1/2阻害剤 (17)
  • 新製品
製品コード 製品名称 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
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.
E1497New Tulmimetostat Tulmimetostat (CPI-0209) is an orally bioavailable and selective inhibitor of EZH2 that has therapeutic potential for androgen receptor-dependent prostate cancer.

EZH1/2阻害剤の選択性比較

Tags: EZH1/2 inhibitors | EZH1/2 modulators | EZH1/2 chemical | EZH1/2 Inhibition