GSK2801

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].

Product Specifications

CAS Number

[1619994-68-1]

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.