BAZ1A-IN-1

BAZ1A-IN-1 is a potent inhibitor of BAZ1A (bromodomain-containing protein). BAZ1A-IN-1 shows a KD value of 0.52 μM against BAZ1A bromodomain. BAZ1A-IN-1 shows good anti-viability activity against cancer cell lines expressing a high level of BAZ1A, but weak or no activity against cancer cells with a low expression level of BAZ1A[1].

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

BAZ1A[1]

BAZ1A-IN-1 (Cpd-2) (0.015-100  μM; 96 hours) exhibits good anti-viability activity against all the four cancer cell lines that have a high expression level of BAZ1A, with IC50 values of 5.08 μM, 4.29 μM, 10.65 μM, and 7.70 μM for THP-1, ZR-75-30, BT474, and H1975 cells, respectively[1]. Cell Viability Assay[1] Cell Line: THP-10 (leukemia), ZR-75-30 (breast cancer), BT474 (breast cancer), H1975 (lung cancer) cells Concentration: 0.015-100  μM Incubation Time: 96 hours Result: Significantly inhibited the viability activity in four cancer cell lines which all expressed high levels of BAZ1A.

[1]. Yang Z, et al. Discovery of BAZ1A bromodomain inhibitors with the aid of virtual screening and activity evaluation. Bioorg Med Chem Lett. 2021;33:127745.