RB-3

RB-3, a PRC1 inhibitor, binds to RING1B-BMI1f, with a Kd of 2.8 μM[1].

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> E1/E2/E3 Enzyme

Kd: 2.8 μM (RING1B-BMI1f)[1].

RB-3 decreases the global level of H2A ubiquitination and induces differentiation in leukemia cell lines and primary acute myeloid leukemia (AML) samples[1]. RB-3 inhibits H2A ubiquitination with an IC50 of 1.6 μM[1]. RB-3 inhibits PRC1 and disrupts the interaction with nucleosomes[1]. RB-3 reduces colony formation in a mixed lineage leukemia (MLL)-eleven nineteen leukemia (ENL) model[1]. Western Blot Analysis[1] Cell Line: TEX cells. Concentration: 6, 12, 25 μM. Incubation Time: 8d. Result: Dose-dependently increased C/EBPα-p42 protein levels.

[1]. Shirish Shukla, et al. Small-molecule inhibitors targeting Polycomb repressive complex 1 RING domain. Nat Chem Biol. 2021 Jul;17(7):784-793.