PBRM1-BD2-IN-5 is a potent PBRM1 Bromodomain inhibitor with Kd values of 1.5 μM and 3.9 μM for PBRM1-BD2 and PBRM1-BD5, respectively, and an IC50 value of 0.26 μM for PBRM1-BD2. PBRM1-BD2-IN-5 reduces the binding of full-length PBRM1 within the PBAF complex in cell lysates to acetylated histone peptide. PBRM1-BD2-IN-5 can be used to research anticancer.
PBRM1-BD2-IN-5 (compound 16) (0-10 μM; 5 days) inhibits PBRM1-expressed LNCaP cells, and reduces the binding of full-length PBRM1 within the PBAF complex in cell lysates to acetylated histone peptides[1].
References:
[1]. Shishodia S, et al. Selective and Cell-Active PBRM1 Bromodomain Inhibitors Discovered through NMR Fragment Screening. J Med Chem. 2022 Oct 13.