GSK503

SKU: orb1307466

Description

GSK503

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.) reduce 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 C57B-/- 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 inhibit 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.
• Disclaimer: For research use only

Alternative Names

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

Compound Identifiers

PubChem CID

67469117