GSK3326595, Selective PRMT5 inhibitor (TBI4028)
$90.00 – $351.00
Selective PRMT5 inhibitor
SKU | Stock | SIZE (mg) | Price | Quantity | ||
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TBI4028-5MG | Yes | 5 MG | $90.00 | |||
TBI4028-25MG | Yes | 25 MG | $351.00 |
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Description
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.
Additional information
SIZE (mg) | 25 MG, 5 MG |
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