PRC1-IN-1 is a PRC1 complex inhibitor. PRC1-IN-1 binds to both RING1A and RING1B proteins, and inhibits the activities of RING1B-BMI1 and RING1B-PCGF1. PRC1-IN-1 effectively inhibits H2AK119 ubiquitination and induces cell differentiation in leukemia cells. PRC1-IN-1 can be used for the research of leukemia [1].
In Vitro, PRC1-IN-1 (compound RB-4) (0-220 μM) binds to RING1B-BMI1, RING1A-BMI1 and RING1B-PCGF1 heterodimers with similarly high affinity, with corresponding KD values of 1.7 μM, 2.0 μM and 1.7 μM[1]. PRC1-IN-1 (0.3-24 μM) inhibits the E3 ligase activity of RING1B-BMI1, RING1A-BMI1 and RING1B-PCGF1 heterodimers in vitro, with IC50 values of 2.8 μM, 2.6 μM and 1.8 μM, respectively[1]. PRC1-IN-1 (3.1-25 μM; 4 days) inhibits global H2A ubiquitination, reduces the expression of the CD34 stem cell marker, and upregulates the expression of the CEBPα differentiation marker in TEX leukemia cells after 4 days of treatment[1].
References:
[1]. Yao Y, et al. Development of PRC1 Inhibitors Employing Fragment-Based Approach and NMR-Guided Optimization. J Med Chem. 2025;68(2):1382-1396.
In Vitro, PRC1-IN-1 (compound RB-4) (0-220 μM) binds to RING1B-BMI1, RING1A-BMI1 and RING1B-PCGF1 heterodimers with similarly high affinity, with corresponding KD values of 1.7 μM, 2.0 μM and 1.7 μM[1]. PRC1-IN-1 (0.3-24 μM) inhibits the E3 ligase activity of RING1B-BMI1, RING1A-BMI1 and RING1B-PCGF1 heterodimers in vitro, with IC50 values of 2.8 μM, 2.6 μM and 1.8 μM, respectively[1]. PRC1-IN-1 (3.1-25 μM; 4 days) inhibits global H2A ubiquitination, reduces the expression of the CD34 stem cell marker, and upregulates the expression of the CEBPα differentiation marker in TEX leukemia cells after 4 days of treatment[1].
References:
[1]. Yao Y, et al. Development of PRC1 Inhibitors Employing Fragment-Based Approach and NMR-Guided Optimization. J Med Chem. 2025;68(2):1382-1396.