LP99

LP99 is a potent inhibitor of the bromodomain containing proteins BRD7 and BRD9 that binds with K_d values of 99 and 909 nM, respectively, as determined by isothermal titration calorimetry.^1,2 It is selective for BRD7/9 over a panel of 48 BRDs at concentrations up to 10 µM determined using differential scanning fluorimetry. It inhibits BRD7 interactions with histones H3.3 and H4 with IC₅₀ values of 3.7 and 3.3 µM, respectively, in a bioluminescence resonance energy transfer (BRET) assay in HEK293 cells. Similarly, it inhibits BRD9 from interacting with H3.3 and H4 with IC₅₀ values of 5.1 and 6.2 µM, respectively. It also decreases the level of IL-6 secreted from LPS-stimulated THP-1 cells. See the Structural Genomics Consortium (SGC) website for more information.

WARNING This product is not for human or veterinary use.

1. Clark, P.G., Vieira, L.C., Tallant, C., et al. LP99: Discovery and synthesis of the first selective BRD7/9 bromodomain inhibitor. Angew. Chem. Int. Ed. Engl. 54(21), 6217-6221 (2015).

2. Karim, R.M., and Schönbrunn, E. An advanced tool to interrogate BRD9. J. Med. Chem. 59(10), 4459-4461 (2016).