GSK2801

SKU: orb1305490

Description

GSK2801 is a potent and selective cell-active inhibitor targeting the BAZ2A (Kd=136 nM) and BAZ2B (Kd=257 nM) bromodomains by competing with acetylated lysine. This tool compound is used in vitro to study bromodomain function in areas such as cancer biology and chromatin remodeling.

Research Area

Cell Biology, Epigenetics & Chromatin

Key Properties

• CAS Number: 1619994-68-1
• MW: 371.45
• Purity: 99.88%
• Formula: C₂₀H₂₁NO₄S
• SMILES: CCCOc1ccn2c(cc(-c3ccccc3S(C)(=O)=O)c2c1)C(C)=O
• Target: Apoptosis,Epigenetic Reader Domain
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.38 mM);DMSO:18.6 mg/mL (50.07 mM)

Bioactivity

• Target IC50:
  BAZ2A:257 nM(Kd)|BAZ2B:136 nM(Kd)
• In Vivo:
  In male CD1 mice, GSK2801 (30 mg/kg, p.o. and i.p.) has reasonable in vivo exposure after oral dosing, modest clearance, and reasonable plasma stability.
• In Vitro:
  In U2OS cells transfected with mutant BAZ2A (N1873F), GSK2801 (1 μM) accelerates FRAP half-recovery time by displacing BAZ2A from chromatin.

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

TNBC, cetyl-lysine, Apoptosis, BAZ2A, BAZ2B, Inhibitor, EpigeneticReaderDomain, Epigenetic Reader Domain, GSK 2801, GSK2801, GSK-2801, inhibit, orally

Compound Identifiers

PubChem CID

73010930