Chemical Name: 6-[(1-Acetylpiperidine-4-yl)amino]-N-[(2S)-3-(3,4-dihydro-1H-isoquinolin-2-yl)-2-hydroxypropyl]pyrimidine-4-carboxamide. Alternate Names: EPZ015938
PRMT5 inhibitor
Molekulargewicht:
452.56
Reinheit:
98% by HPLC NMR (Conforms)
Formulierung:
Off-white solid
CAS Nummer:
[1616392-22-3]
Formel:
C24H32N6O3
Anwendungsbeschreibung:
GSK3326595 is a potent (IC50 = 6.2nM), selective (>4000-fold over 20 other methyltransferases), SAM uncompetitive, peptide competitive inhibitor of PRMT5.1 PRMT5 inhibition activated the p53 pathway via induction of alternative splicing of MDM4 leading to a potent anti-proliferative response both in vitro and in vivo. Combination therapy with palbociclib (CDK4/6 inhibitor, Focus Cat. 10-4760) and GSK3326595 lead to increased efficacy of palbociclib in treating native and resistant models of melanoma via regulation of the PRMT5-MDM4 axis.2 Currently in clinical Trials.3
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