PBRM1-BD2-IN-5

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[1].

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

Kd: 1.5 μM (PBRM1-BD2), 3.9 μM (PBRM1-BD5)[1] IC50: 0.26 μM (PBRM1-BD2)[1]

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]. Cell Viability Assay[1] Cell Line: LNCaP cells expressing lentiviral shPBRM1 Concentration: 0, 0.1, 1 and 10 μM Incubation Time: 5 days Result: Exhibited a more significant effect on LNCaP viability in cells with native PBRM1 levels than in cells with PBRM1 knockdown. Reduced the binding of full-length PBRM1 within the PBAF complex in cell lysates to acetylated histone peptides.