GSK3326595
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- Application
- Inhibition (Inh)
- Fonction
- Selective PRMT5 inhibitor
- Attributs du produit
- 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.
- Pureté
- >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)
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- Restrictions
- For Research Use only
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- Format
- Powder
- Stock
- -20 °C
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- Sujet
- EPZ015938,Proliferation,Epigenetics,Posttranslational modification,Protein methyltransferase,RNA,Cancer,Chromatin,p53
- Poids moléculaire
- 452.56
- Numéro CAS
- 1616392-22-3
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