GSK3326595, Selective PRMT5 inhibitor

Product Details

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

Alternate Names: EPZ015938

Molecular Formula: C₂₄H₃₂N₆O₃

Formula Weight: 452.56

CAS Number: 1616392-22-3

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 20 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

Applications

Selective PRMT5 inhibitor

Functions

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, 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.  Currently in clinical Trials.

Application Procedures

First dissolved in DMSO (up to 20 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20° for up to 1 month.

Research use only.

Documents

• Datasheet (PDF)
• MSDS (PDF)