Biological Activity
UMB298 is a potent and selective CBP/P300 bromodomain inhibitor[1].
UMB298 (0.01~10 μM; 50 days; MOLM13 and MM cells) inhibits cells growth[1].UMB298 (1~10 μM; 2 hours; MOLM13 cells) reduces the H3K27ac level similar to CBP30 and causes MYC depletion as a signature of CBP inhibition in acute myeloid leukemia[1].UMB298 (3 μM; 2hours; MOLM13 cells) down-regulates MYC expression[1].
References
[1]. Muthengi A, et al. Development of Dimethylisoxazole-Attached Imidazo[1,2-a]pyridines as Potent and Selective CBP/P300 Inhibitors. J Med Chem. 2021;64(9):5787-5801.
