EZH1/2
- Inhibitory Selectivity
- Solubility
| Catalog No. | Product Name | Solubility(25°C) | ||
|---|---|---|---|---|
| Water | DMSO | Alcohol | ||
| S7004 | EPZ005687 | <1 mg/mL | 2 mg/mL | <1 mg/mL |
| S7164 | GSK343 | <1 mg/mL | 1 mg/mL | 4 mg/mL |
| S7128 | Tazemetostat (EPZ-6438) | <1 mg/mL | 5 mg/mL | <1 mg/mL |
| S7165 | UNC1999 | <1 mg/mL | 20 mg/mL | 50 mg/mL |
| S8353 | CPI-1205 | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S7805 | EPZ011989 | <1 mg/mL | <1 mg/mL | 100 mg/mL |
| S8494 | PF-06726304 | <1 mg/mL | 10 mg/mL | 22 mg/mL |
| S7611 | EI1 | <1 mg/mL | 42 mg/mL | <1 mg/mL |
| S7804 | GSK503 | <1 mg/mL | 100 mg/mL | 26 mg/mL |
| S7061 | GSK126 | <1 mg/mL | 3 mg/mL | <1 mg/mL |
| S7656 | CPI-360 | <1 mg/mL | 20 mg/mL | 18 mg/mL |
| S7616 | CPI-169 | <1 mg/mL | 100 mg/mL | 100 mg/mL |
- EZH1/2 Inhibitors (13)
- New EZH1/2 Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S7004 |
EPZ005687EPZ005687 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. |
Western blot analysis of day 7 lysates from LX92 lysates treated with various EZH2 inhibitors. |
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| S7164 |
GSK343GSK343 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. |
Representative confocal microscopy images of oocytes with DZNep or GSK343 treatment. The oocytes presented with a typical barrel-shaped spindle and well-aligned chromosomes on the metaphase plate not only in DZNep or GSK343 treated group but also in the control group. Spindle was recognized by α-tubulin (green) and DNA was recognized by PI (Propidium iodide, red). Scale bar = 4 μm.
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| S7128 |
Tazemetostat (EPZ-6438)Tazemetostat (EPZ-6438) 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. |
we examined the E-cadherin, ZEB1 and Snail expressions after using EZH2 RNAi, DZNeP and EPZ-6438. “*”represent P<0.05 when compared with control group.
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| S7165 |
UNC1999UNC1999 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. |
Ex vivo growth of the SCLC PDX LX92 is significantly inhibited by the EZH2 inhibitors EPZ-5687, GSK343 and UNC1999 as measured by resazurin conversion (two-way analysis of variance, adjusted for multiple comparisons by the method of Dunnet).
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| S8607New |
JQ-EZ-05 (JQEZ5)JQ-EZ-05 is a specific and reversible EZH1/2 inhibitor. |
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| S8353 |
CPI-1205CPI-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. |
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| S7805 |
EPZ011989EPZ011989 is a potent, selective, orally bioavailable EZH2 inhibitor with Ki of <3 nM. |
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| S8494 |
PF-06726304PF-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. |
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| S7611 |
EI1EI1 is a potent and selective EZH2 inhibitor with IC50 of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively. |
EZH2 inhibitors EI1 or GSK343 are applied in MDA-MB-231 breast cancer cells with NBAT1 over-expression. The invasion suppression effects of NBAT1 was reversed by concomitant EZH2 inhibitors. |
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| S7804 |
GSK503GSK503 is a potent and specific EZH2 methyltransferase inhibitor. |
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| S7061 |
GSK126GSK126 is a potent, highly selective EZH2 methyltransferase inhibitor with IC50 of 9.9 nM, >1000-fold selective for EZH2 over 20 other human methyltransferases. |
HeLa cells were transfected with NS (nonspecific) or EZH2-specific siRNA for 48 h with protease inhibitors (10 μM E64 and 10 μM pepstatin-A). Cells were stained with LC3B antibody (green) and DAPI, and observed under confocal microscopy for LC3B puncta. Scale bars: 10 μm
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| S7656 |
CPI-360CPI-360 is a potent, selective,and SAM-competitive EZH1 inhibitor with IC50 of 102.3 nM, >100-fold selectivity over other methyltransferases. |
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| S7616 |
CPI-169CPI-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. |
