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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
产品编号 ABIN7233257
发货至: 中国
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Quick Overview for GSK3326595 (ABIN7233257)

应用范围

Inhibition (Inh)

Chemical Name

6-[(1-Acetylpiperidine-4-yl)amino]-N-[(2S)-3-(3,4-dihydro-1H-isoquinolin-2-yl)-2-hydroxypropyl]pyrimidine-4-carboxamide
  • 原理

    Selective PRMT5 inhibitor

    产品特性

    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.

    纯度

    >98 %

    Formula

    C24H32N6O3

    Solubility

    Soluble in DMSO (up to 20 mg/ml)
  • 限制

    仅限研究用
  • 状态

    Powder

    储存条件

    -20 °C
  • 背景

    EPZ015938,Proliferation,Epigenetics,Posttranslational modification,Protein methyltransferase,RNA,Cancer,Chromatin,p53

    分子量

    452.56

    CAS-编号

    1616392-22-3
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