UMB298

UMB298 is a potent and selective CBP/P300 bromodomain inhibitor[1].

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

BRD4:5193 nM (IC50)

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]. Cell Viability Assay[1] Cell Line: MOLM13 and MM cells Concentration: 0.01~10 μM Incubation Time: 50 days Result: Inhibited cells growth. Western Blot Analysis[1] Cell Line: MOLM13 cells Concentration: 1~10 μM Incubation Time: 2 hours Result: Reduced the H3K27ac level similar to CBP30 and caused MYC depletion as a signature of CBP inhibition in acute myeloid leukemia. RT-PCR[1] Cell Line: MOLM13 cells Concentration: 3 μM Incubation Time: 2 hours Result: Down-regulated MYC expression.

[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.