Welcome to Shanghai Probechem Biochemicals Co Ltd !Global Supplier of Chemical Probes, Inhibitors & Agonists.
Chemical Structure : SKLB-03176
Catalog No.: PC-72287Not For Human Use, Lab Use Only.
SKLB-03176 (SKLB03176) is a potent, selective, covalent EZH2 inhibitor with IC50 of 47 nM, covalently binds to the SAM pocket of EZH2.
Bulk size, bulk discount!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
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.
| M.Wt | 514.63 | |
| Formula | C29H34N6O3 | |
| Appearance | Solid | |
| Storage |
|
|
| Solubility |
|
|
1. Zhang Q, et al. Biomed Pharmacother. 2022 Mar;147:112617.
Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright
