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Chemical Structure : MS177
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.
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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 | |
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1. Jun Wang, et al. Nat Cell Biol. 2022 Feb 24. doi: 10.1038/s41556-022-00850-x.
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