Welcome to ProbeChem!Global Supplier of Chemical Probes, Inhibitors & Agonists.
Chemical Structure : MS177
CAS No.: 2225938-86-1
Catalog No.: PC-72286Not For Human Use, Lab Use Only.
MS177 (MS-177) is a potent and selective EZH2 degarder (PROTAC) based on EZH2 inhibitor C24 with CRBN ligand pomalidomide with DC50 of 0.2 uM in EOL-1 cells.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 2 mg | $128 | In stock | |
| 5 mg | $198 | In stock | |
| 10 mg | $298 | In stock | |
| 50 mg | $488 | In stock | |
| 100 mg | Get quote |
Bulk size, bulk discount!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
MS177 (MS-177) is a potent and selective EZH2 degarder (PROTAC) based on EZH2 inhibitor C24 with CRBN ligand pomalidomide with DC50 of 0.2 uM in EOL-1 cells.
MS177 effectively degraded cellular EZH2-PRC2, suppressed global H3K27me3 in leukaemia cells.
MS177 exhibited half-maximal degradation concentration (DC50) values of 0.2 ± 0.1 μM and 1.5 ± 0.2 μM, and maximum degradation (Dmax) values of 82% and 68%, respectively, in EOL-1 and MV4;11 cells.
MS177 efficiently suppresses EZH2-PRC2 functions, also efficiently induces Myc degradation in cancer cells, suppresses EZH2-PRC2 functions.
MS177 efficiently induces leukaemia cell growth inhibition, apoptosis and cell cycle progression arrest, which is more effective than EZH2 inhibitors. MS177 (i.p. injection, 50-100 mg/kg) represses AML growth without apparent toxicity in PDX models.
| M.Wt | 914.037 | |
| Formula | C48H55N11O8 | |
| Appearance | Solid | |
| Storage |
|
|
| Solubility |
10 mM in DMSO |
|
| Chemical Name/SMILES |
N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(6-(4-(2-(3-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethoxy)propanamido)ethyl)piperazin-1-yl)pyridin-3-yl)-1-isopropyl-1H-indazole-4-carboxamide |
|
1. Jun Wang, et al. Nat Cell Biol. 2022 Feb 24. doi: 10.1038/s41556-022-00850-x.
Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright
