纯度:98% by HPLC;NMR (Conforms)
分子式:C24H32N6O3
分子量:452.56
溶剂:DMSO (20 mg/ml)
性状:Off-white solid
存储:-20°C
Activity (short version):PRMT5 inhibitor
Function / Pharmacology: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