GSK3326595
Quick Overview for GSK3326595 (ABIN7233257)
Application
Chemical Name
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Purpose
- Selective PRMT5 inhibitor
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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.
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Purity
- >98 %
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Formula
- C24H32N6O3
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Solubility
- Soluble in DMSO (up to 20 mg/ml)
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Restrictions
- For Research Use only
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Format
- Powder
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Storage
- -20 °C
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Background
- EPZ015938,Proliferation,Epigenetics,Posttranslational modification,Protein methyltransferase,RNA,Cancer,Chromatin,p53
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Molecular Weight
- 452.56
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CAS-No
- 1616392-22-3
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