PBRM1-BD2-IN-1

PBRM1-BD2-IN-1 is a selective and cell-active polybromo-1 (PBRM1) bromodomain inhibitor. PBRM1-BD2-IN-1 has binding affinity and inhibitory activity for PBRM1-BD2 with Kd and IC50 values of 0.7 μM and 0.2 μM, respectively. PBRM1-BD2-IN-1 can be used for the research of cancer[1].

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

Kd: 0.7 μM (PBRM1-BD2), 0.35 μM (PBRM1-BD5), 8.1 μM (SMARCA2B), 5.0 μM (SMARCA4) [1]. IC50: 0.2 μM (PBRM1-BD2)[1].

PBRM1-BD2-IN-1 (0, 0.1, 1, and 10 μM; 5 days) selectively inhibit growth of a PBRM1-dependent prostate cancer cell line[1]. PBRM1-BD2-IN-1 has binding affinity for PBRM1-BD2, PBRM1-BD5, SMARCA2B amd SMARCA4 with Kd values of 0.7 μM, 0.35 μM, 8.1 μM and 5.0 μM, respectively[1]. PBRM1-BD2-IN-1 has inhibitory activity for PBRM1-BD2 with IC50 value of 0.2 μM[1]. Cell Viability Assay[1] Cell Line: Human prostate cell lines LNCaP, PC3, and RWPE-1 Concentration: 0, 0.1, 1, and 10 μM Incubation Time: 5 days Result: Inhibited LNCaP growth at higher concentrations.