MS177

Biorbyt

MS177

10

Research Use Only

C48H55N11O8

914.02

MS 177 (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 microM and 1.5 +/- 0.2 microM, 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, 50-1 g/kg) represses AML growth without apparent toxicity in PDX models.

N1(C(C)C)C2=C(C(C(NCC3=C(C)C=C(C)NC3=O)=O)=CC(C3=CC=C(N4CCN(CCNC(=O)CCOCCNC5=CC=CC6=C5C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)N=C3)=C2)C=N1

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