DATASHEET
Formulation
Pale yellow to off-white solid
Storage:
-20°C
Product Information:
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
Description:
CAS Number: 1616392-22-3<br></br>Chemical Name: 6-[(1-Acetylpiperidine-4-yl)amino]-N-[(2S)-3-(3,4-dihydro-1H-isoquinolin-2-yl)-2-hydroxypropyl]pyrimidine-4-carboxamide <br></br>Molecular weight: 452.56<br></br>Formula: C24H32N6O3<br></br>Solubility: DMSO (20 mg/ml)<br></br>Physical Properties: Off-white solid<br></br>Purity: 98% by HPLC NMR (Conforms)