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GSK3326595

Inh 1616392-22-3 6-[(1-Acetylpiperidine-4-yl)amino]-N-[(2S)-3-(3,4-dihydro-1H-isoquinolin-2-yl)-2-hydroxypropyl]pyrimidine-4-carboxamide
Catalog No. ABIN7233257
  • Application
    Inhibition (Inh)
    Purpose
    Selective PRMT5 inhibitor
    Characteristics
    GSK3326595 is a potent (IC50 = 6.2nM), selective (>4000-fold over 20 other methyltransferases), SAM uncompetitive, peptide competitive inhibitor of PRMT5. 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) and GSK3326595 lead to increased efficacy of palbociclib in treating native and resistant models of melanoma via regulation of the PRMT5-MDM4 axis. Currently in clinical Trials.
    Purity
    >98 %
    Chemical Name
    6-[(1-Acetylpiperidine-4-yl)amino]-N-[(2S)-3-(3,4-dihydro-1H-isoquinolin-2-yl)-2-hydroxypropyl]pyrimidine-4-carboxamide
    Formula
    C24H32N6O3
    Solubility
    Soluble in DMSO (up to 20 mg/ml)
  • Restrictions
    For Research Use only
  • Format
    Powder
    Storage
    -20 °C
  • Background
    EPZ015938,Proliferation,Epigenetics,Posttranslational modification,Protein methyltransferase,RNA,Cancer,Chromatin,p53
    Molecular Weight
    452.56
    CAS-No
    1616392-22-3
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