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EZH1/2
EZH1/2 Products
- All (19)
- EZH1/2 Inhibitors (19)
- New EZH1/2 Products
| Catalog No. | Product Name | Information | Product Use Citations | Product Validations |
|---|---|---|---|---|
| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| S7805 | EPZ011989 | EPZ011989 is a potent, selective, orally bioavailable EZH2 inhibitor with Ki of <3 nM. | ||
| 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. | ||
| 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. | ||
| S7804 | GSK503 | GSK503 is a potent and specific EZH2 methyltransferase inhibitor. |
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| 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. |
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| 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. | ||
| S8926 | Valemetostat (DS-3201) | Valemetostat (DS-3201, DS-3201b) is a selective EZH1/2 dual inhibitor. | ||
| 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. | ||
| S8607 | JQ-EZ-05 (JQEZ5) | JQ-EZ-05 (JQEZ5) is a specific and reversible EZH1/2 inhibitor. | ||
| E4850New | 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 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. | ||
| S9655New | 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 | 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) is a potent, highly selective EZH2 methyltransferase inhibitor with IC50 of 9.9 nM, >1000-fold selective for EZH2 over 20 other human methyltransferases. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| S7805 | EPZ011989 | EPZ011989 is a potent, selective, orally bioavailable EZH2 inhibitor with Ki of <3 nM. | ||
| 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. | ||
| 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. | ||
| S7804 | GSK503 | GSK503 is a potent and specific EZH2 methyltransferase inhibitor. |
|
|
| 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. |
|
|
| 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. | ||
| S8926 | Valemetostat (DS-3201) | Valemetostat (DS-3201, DS-3201b) is a selective EZH1/2 dual inhibitor. | ||
| 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. | ||
| S8607 | JQ-EZ-05 (JQEZ5) | JQ-EZ-05 (JQEZ5) is a specific and reversible EZH1/2 inhibitor. | ||
| E4850New | 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 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. | ||
| S9655New | 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 | Tulmimetostat (CPI-0209) is an orally bioavailable and selective inhibitor of EZH2 that has therapeutic potential for androgen receptor-dependent prostate cancer. | ||
| E4850New | 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. | ||
| S9655New | 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. |
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Tags: EZH1/2 inhibitors | EZH1/2 modulators | EZH1/2 chemical | EZH1/2 Inhibition
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