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GSK097

Names

[ CAS No. ]:
2159137-02-5

[ Name ]:
GSK097

Biological Activity

[Description]:

GSK097 is a potent and selective Inhibitor of the second bromodomain (BD2) of the bromodomain and extra-terminal domain (BET) proteins. GSK097 displays 2000-fold selective for BD2 over BD1 (BRD4 data) with >1 mg/mL solubility in FaSSIF media[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

[In Vitro]

GSK097 displays pIC50s 7.4, 8.0, 7.6, and 7.9 for BRD2 BD2, BRD3 BD2, BRD4 BD2 and BRDT BD2, respectively[1].

[References]

[1]. Harrison LA, et al. Identification of a Series of N-Methylpyridine-2-carboxamides as Potent and Selective Inhibitors of the Second Bromodomain (BD2) of the Bromo and Extra Terminal Domain (BET) Proteins [published online ahead of print, 2021 Jul 7]. J Med Chem. 2021;10.1021/acs.jmedchem.0c02155.

Chemical & Physical Properties

[ Molecular Formula ]:
C19H21N3O3

[ Molecular Weight ]:
339.39

Related Compounds