GSK591

SKU: orb1300406

Description

GSK591 (EPZ015866) is a potent and selective PRMT5 inhibitor with an IC50 of 11 nM. It is a valuable chemical probe for investigating PRMT5 biology in cancer research, demonstrating utility in both in vitro cellular assays and in vivo preclinical models of hematologic malignancies.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1616391-87-7
• MW: 380.48
• Purity: 99.77% (May vary between batches)
• Formula: C₂₂H₂₈N₄O₂
• SMILES: O[C@@H](CNC(=O)c1ccnc(NC2CCC2)c1)CN1CCc2ccccc2C1
• Target: Histone Methyltransferase
• Solubility: DMSO:60 mg/mL (157.7 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.26 mM)

Bioactivity

• Target IC50:
  PRMT5:11 nM
• In Vitro:
  In an in vitro biochemical assay, GSK591 potently inhibits the PRMT5/MEP50 complex from methylating (histone) H4 with IC50 = 11 nM. In Z-138 cells, GSK591 inhibits the symmetric arginine methylation of SmD3 with EC50 = 56 nM. Further, GSK591 is selective for PRMT5 (up to 50 micromolar) relative to a panel of methyltransferases.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

HistoneMethyltransferase, Histone Methyltransferase, Inhibitor, GSK591, GSK-591, GSK 591, GSK 3203591, GSK3203591, GSK-3203591, EPZ015866, EPZ-015866, EPZ 015866, inhibit, PRMT5

Compound Identifiers

PubChem CID

117072552