2396639-11-3

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

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

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