PBRM1-BD2-IN-2 is a selective and cell-active polybromo-1 (PBRM1) bromodomain inhibitor. PBRM1-BD2-IN-2 has binding affinity and inhibitory activity for PBRM1-BD2 with Kd and IC50 values of 9.3 μM and 1.0 μM, respectively. PBRM1-BD2-IN-2 can be used for the research of cancer.
PBRM1-BD2-IN-2 (0, 0.1, 1, and 10 μM; 5 days) selectively inhibit growth of a PBRM1-dependent prostate cancer cell line[1].PBRM1-BD2-IN-2 has binding affinity for PBRM1-BD2, PBRM1-BD5, SMARCA2B amd SMARCA4 with Kd values of 9.3 μM, 10.1 μM, 18.4 μM and 69 μM, respectively[1].PBRM1-BD2-IN-2 has inhibitory activity for PBRM1-BD2 with IC50 value of 1.0 μM[1].
References:
[1]. Shifali Shishodia, et al. Selective and Cell-Active PBRM1 Bromodomain Inhibitors Discovered through NMR Fragment Screening. J Med Chem. 2022 Oct 13.