GSK2801

• Description :

  GSK2801, a chemical probe, is a potent, selective, orally active and cell active acetyl-lysine competitive BAZ2A and BAZ2B bromodomains inhibitor with Kd values of 136 nM and 257 nM, respectively. GSK2801 shows >50-fold selectivity for BAZ2A/B over BRD4[1].

• UNSPSC :

  12352005

• Hazard Statement :

  H302, H315, H319, H335

• Target :

  Apoptosis; Epigenetic Reader Domain

• Type :

  Reference compound

• Related Pathways :

  Apoptosis; Epigenetics

• Applications :

  Cancer-programmed cell death

• Field of Research :

  Cancer

• Assay Protocol :

  https://www.medchemexpress.com/GSK2801.html

• Purity :

  99.95

• Solubility :

  DMSO : 50 mg/mL (ultrasonic)

• Smiles :

  O=C(C)C1=CC(C2=C(S(=O)(C)=O)C=CC=C2)=C3N1C=CC(OCCC)=C3

• Molecular Formula :

  C20H21NO4S

• Molecular Weight :

  371.45

• Precautions :

  H302, H315, H319, H335

• References & Citations :

  [1]Chen P, et al. Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B. J Med Chem. 2016 Feb 25;59 (4) :1410-24.|[2]Bevill SM, et al. GSK2801, a BAZ2/BRD9 Bromodomain Inhibitor, Synergizes with BET Inhibitors to Induce Apoptosis in Triple-Negative Breast Cancer. Mol Cancer Res. 2019 Jul;17 (7) :1503-1518.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• CAS Number :

  [1619994-68-1]