GSK973

GSK973, a chemical probe, is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family, with a pIC50 of 7.8 and a pKd of 8.7 for BRD4 BD2. GSK973 displays a 1600-fold selectivity for BRD4 BD2 over BRD4 BD1. GSK973 shows good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2 (pIC50=7.4~7.8; pKd=8.3~8.5) [1].

Product Specifications

CAS Number

[2138473-38-6]

UNSPSC

12352005

Target

Epigenetic Reader Domain

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/gsk973.html

Purity

99.97

Solubility

DMSO : 125 mg/mL (ultrasonic)

Smiles

[H][C@]1([C@@H]2NC(C3=CC(C(NC)=O)=C4C([C@@H]([C@H](O4)CF)C5=CC=CC=C5)=C3)=O)[C@]2([H])COC1

Molecular Formula

C23H23FN2O4

Molecular Weight

410.44

References & Citations

[1]Preston A, et al. GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family. ACS Med Chem Lett. 2020;11 (8) :1581-1587. Published 2020 Jul 6.