NI-42

Description: NI-42 is a structurally orthogonal chemical probe for the BRPFs and is biased. It effective inhibitor of the BRD of the BRPFs (IC50s of BRPF1/2/3=7.9/48/260 nM, Kds of BRPF1/2/3=40/210/940 nM). It also has excellent selectivity over nonclass IV BRD proteins. Target: Epigenetic Reader Domain. Smiles: Cc1cc2cc(NS(=O)(=O)c3ccc(cc3)C#N)ccc2n(C)c1=O. References: Igoe N, et al. Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies. J Med Chem. 2017 Jan 26,60(2):668-680.