| Name | SKLB-03176 | CAS# | 2609675-22-9 | |
|---|---|---|---|---|
| Price | $500.0/5mg | Purity | 98.0% | |
| Stocking Period |
3 Day | Stock | 3 | |
| Product Webpage: | https://www.dcchemicals.com/product_show-sklb-03176.html | |||
| Detail
Product Information
SKLB-03176 (SKLB03176) is a potent, selective, covalent EZH2 inhibitor with IC50 of 47 nM, covalently binds to the SAM pocket of EZH2.SKLB-03176 showed good inhibitory activity against mutations EZH2 Y641F, EZH2 Y641N, and EZH2A677G at 200 nM concentration.SKLB-03176 exhibited weak activity against other targets, such as 5 histone methyltransferases and more than 30 kinases, >50-fold selective for EZH2 over the highly homologous H3K27 methyltransferase EZH1 (IC50=2.45 uM).SKLB-03176 inhibited the activity of a variety of EZH2 mutants and significantly inhibited the expression of H3K27Me3 in cells.SKLB-03176 showed no cytotoxicity to normal cells. |