EZH1/2

亜型選択性的な製品

EZH1/2製品

  • All (22)
  • EZH1/2阻害剤 (21)
  • 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。
Theranostics, 2025, 15(14):7127-7153
EMBO J, 2025, 10.1038/s44318-025-00537-7
EBioMedicine, 2025, 119:105879
GSK126-S706101W0120170825.gif
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 Cancer, 2025, 10.1038/s43018-025-00960-z
Nat Cell Biol, 2025, 27(9):1411-1421
Nat Commun, 2025, 16(1):5387
EPZ-6438-S712801W0120181210.gif
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.
Cell, 2025, S0092-8674(25)00396-4
Research (Wash D C), 2025, 8:0602
Mol Genet Genomics, 2025, 300(1):63
GSK343-S716401Y0420170213.gif
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.
Cell Stem Cell, 2025, S1934-5909(25)00041-4
Cell Rep, 2025, 44(5):115673
bioRxiv, 2025, 2025.05.22.655558
UNC1999-S716501Z1520150908.gif
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.
Commun Biol, 2024, 7(1):1535
J Exp Clin Cancer Res, 2023, 42(1):320
BMC Med, 2022, 20(1):189
EPZ005687-S700401W0220161101.gif
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
Sci Adv, 2024, 10(13):eadk4423
S8353 Lirametostat (CPI-1205) Lirametostat (CPI-1205) is an orally available selective inhibitor of the histone lysine methyltransferase EZH2, with potential antineoplastic activity.
Sci Adv, 2024, 10(13):eadk4423
JCI Insight, 2022, e155899
Cancer Discov, 2021, candisc.0913.2020
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
J Exp Clin Cancer Res, 2023, 42(1):96
Nat Commun, 2022, 13(1):6226
S7804 GSK503 GSK503 is a potent and specific EZH2 methyltransferase inhibitor.
JCI Insight, 2025, e177545
Int J Mol Sci, 2023, 24(10)8603
Cancer Res, 2022, CAN-22-0736
GSK503-S780401W0320181228.gif
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.
NPJ Precis Oncol, 2025, 9(1):7
Cancer Res, 2018, 78(20):5731-5740
Elife, 2018, 7e35368
EI1-S761101Z0520161110.gif
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.
NPJ Precis Oncol, 2025, 9(1):7
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.
Cell Rep Med, 2025, S2666-3791(25)00102-8
NPJ Precis Oncol, 2025, 9(1):69
Commun Biol, 2025, 8(1):269
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
F0281 Ezh2 Antibody [M10N8] Ezh2 Rabbit mAb detects endogenous levels of total Ezh2 protein. This antibody does not cross-react with Ezh1 protein.
E1521New SHR2554 SHR2554 is an inhibitor of EZH2. SHR2554 exhibits anti-tumor activity with IC50 values ranging from 0.365 to 3.001 μM in a dose-dependent manner, in T-cell lymphoma (TCL) by reducing H3K27me3 levels.
E4678New EZH2/HSP90-IN-29 EZH2/HSP90-IN-29 is a potent dual inhibitor of EZH2 and HSP90, with IC50s of 6.29 nM and 60.1 nM, for EZH2 and HSP90, respectively, that induces M-phase cell cycle arrest, promotes apoptosis/necrosis-related gene expression, and inhibits ROS catabolism. It crosses the blood-brain barrier and can show potential as a tractable anti-GBM agent for glioblastoma research.
E4850 Tazemetostat hydrobromide Tazemetostat hydrobromide (EPZ-6438 hydrobromide) is a potent, selective, and orally available inhibitor of EZH2. It inhibits EZH2 with IC50 values of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat hydrobromide also inhibits EZH1 with an IC50 of 392 nM.
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.
Cancer Biol Ther, 2024, 25(1):2427374
Chem Biol Interact, 2023, 382:110602
Oncotarget, 2021, 12(6):549-561
S9655 PF-06821497 PF-06821497 is a selective and orally active inhibitor of Zeste Homolog 2 (EZH2) with a Ki value <0.1 nM against mutant Y641N EZH2. It exhibits robust tumor growth inhibition.
S8702 EBI-2511 EBI-2511 is a highly potent and orally active EZH2 inhibitor with an IC50 of 4 nM for EZH2(A667G).
E1497 Tulmimetostat (CPI-0209) Tulmimetostat (CPI-0209) is an orally bioavailable and selective inhibitor of EZH2 that has therapeutic potential for androgen receptor-dependent prostate cancer.
bioRxiv, 2025, 2025.07.07.663486
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。
Theranostics, 2025, 15(14):7127-7153
EMBO J, 2025, 10.1038/s44318-025-00537-7
EBioMedicine, 2025, 119:105879
GSK126-S706101W0120170825.gif
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 Cancer, 2025, 10.1038/s43018-025-00960-z
Nat Cell Biol, 2025, 27(9):1411-1421
Nat Commun, 2025, 16(1):5387
EPZ-6438-S712801W0120181210.gif
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.
Cell, 2025, S0092-8674(25)00396-4
Research (Wash D C), 2025, 8:0602
Mol Genet Genomics, 2025, 300(1):63
GSK343-S716401Y0420170213.gif
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.
Cell Stem Cell, 2025, S1934-5909(25)00041-4
Cell Rep, 2025, 44(5):115673
bioRxiv, 2025, 2025.05.22.655558
UNC1999-S716501Z1520150908.gif
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.
Commun Biol, 2024, 7(1):1535
J Exp Clin Cancer Res, 2023, 42(1):320
BMC Med, 2022, 20(1):189
EPZ005687-S700401W0220161101.gif
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
Sci Adv, 2024, 10(13):eadk4423
S8353 Lirametostat (CPI-1205) Lirametostat (CPI-1205) is an orally available selective inhibitor of the histone lysine methyltransferase EZH2, with potential antineoplastic activity.
Sci Adv, 2024, 10(13):eadk4423
JCI Insight, 2022, e155899
Cancer Discov, 2021, candisc.0913.2020
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
J Exp Clin Cancer Res, 2023, 42(1):96
Nat Commun, 2022, 13(1):6226
S7804 GSK503 GSK503 is a potent and specific EZH2 methyltransferase inhibitor.
JCI Insight, 2025, e177545
Int J Mol Sci, 2023, 24(10)8603
Cancer Res, 2022, CAN-22-0736
GSK503-S780401W0320181228.gif
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.
NPJ Precis Oncol, 2025, 9(1):7
Cancer Res, 2018, 78(20):5731-5740
Elife, 2018, 7e35368
EI1-S761101Z0520161110.gif
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.
NPJ Precis Oncol, 2025, 9(1):7
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.
Cell Rep Med, 2025, S2666-3791(25)00102-8
NPJ Precis Oncol, 2025, 9(1):69
Commun Biol, 2025, 8(1):269
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
E1521New SHR2554 SHR2554 is an inhibitor of EZH2. SHR2554 exhibits anti-tumor activity with IC50 values ranging from 0.365 to 3.001 μM in a dose-dependent manner, in T-cell lymphoma (TCL) by reducing H3K27me3 levels.
E4678New EZH2/HSP90-IN-29 EZH2/HSP90-IN-29 is a potent dual inhibitor of EZH2 and HSP90, with IC50s of 6.29 nM and 60.1 nM, for EZH2 and HSP90, respectively, that induces M-phase cell cycle arrest, promotes apoptosis/necrosis-related gene expression, and inhibits ROS catabolism. It crosses the blood-brain barrier and can show potential as a tractable anti-GBM agent for glioblastoma research.
E4850 Tazemetostat hydrobromide Tazemetostat hydrobromide (EPZ-6438 hydrobromide) is a potent, selective, and orally available inhibitor of EZH2. It inhibits EZH2 with IC50 values of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat hydrobromide also inhibits EZH1 with an IC50 of 392 nM.
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.
Cancer Biol Ther, 2024, 25(1):2427374
Chem Biol Interact, 2023, 382:110602
Oncotarget, 2021, 12(6):549-561
S9655 PF-06821497 PF-06821497 is a selective and orally active inhibitor of Zeste Homolog 2 (EZH2) with a Ki value <0.1 nM against mutant Y641N EZH2. It exhibits robust tumor growth inhibition.
S8702 EBI-2511 EBI-2511 is a highly potent and orally active EZH2 inhibitor with an IC50 of 4 nM for EZH2(A667G).
E1497 Tulmimetostat (CPI-0209) Tulmimetostat (CPI-0209) is an orally bioavailable and selective inhibitor of EZH2 that has therapeutic potential for androgen receptor-dependent prostate cancer.
bioRxiv, 2025, 2025.07.07.663486
E1521New SHR2554 SHR2554 is an inhibitor of EZH2. SHR2554 exhibits anti-tumor activity with IC50 values ranging from 0.365 to 3.001 μM in a dose-dependent manner, in T-cell lymphoma (TCL) by reducing H3K27me3 levels.
E4678New EZH2/HSP90-IN-29 EZH2/HSP90-IN-29 is a potent dual inhibitor of EZH2 and HSP90, with IC50s of 6.29 nM and 60.1 nM, for EZH2 and HSP90, respectively, that induces M-phase cell cycle arrest, promotes apoptosis/necrosis-related gene expression, and inhibits ROS catabolism. It crosses the blood-brain barrier and can show potential as a tractable anti-GBM agent for glioblastoma research.