GSK503

SKU: orb1307466

Description

GSK-503 is a potent and selective small molecule inhibitor of EZH2, demonstrating antitumor activity in preclinical studies. It is widely used in epigenetic research to investigate histone methylation's role in cancer, with applications in both in vitro cellular assays and in vivo animal models for oncology.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1346572-63-1
• MW: 526.67
• Purity: 99.54%
• Formula: C₃₁H₃₈N₆O₂
• SMILES: CC(C)n1cc(C)c2c(cc(cc12)-c1ccc(nc1)N1CCN(C)CC1)C(=O)NCc1c(C)cc(C)[nH]c1=O
• Target: Histone Methyltransferase
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.27 mM);DMSO:93 mg/mL (176.58 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:25 mg/mL (47.47 mM)

Bioactivity

• Target IC50:
  EZH2:8 nM
• In Vivo:
  In C57BL6 mice immunized with SRBC, GSK503 (150 mg/kg, i.p.) reduced the level of H3K27me3 in splenocytes. In male SCID mice bearing SUDHL4 and SUDHL6 tumors, GSK503 (150 mg/kg, i.p.) inhibits tumor growth. In C57Bl/6 mice bearing murine B16-F10 tumors, GSK503 (150 mg/kg, i.p.) significantly reduces global H3K27me3 levels, inhibits tumor growth and virtually abolishes metastases formation.
• In Vitro:
  GSK503 inhibits the methyltransferase activity of both WT and mutant EZH2 with similar potency. In a panel of seven DLBCL cell lines, GSK503 causes growth inhibition, with enhanced effects when combined with ABT737 or Obatoclax.

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

inhibit, Histone Methyltransferase, HistoneMethyltransferase, Inhibitor, EZH2, GSK503, GSK-503, GSK 503

Compound Identifiers

PubChem CID

67469117