BCOR-PCGF1 inhibitor iBP is a selective PRC1.1 inhibitor, specifically inhibits the interaction between BCOR and PCGF1 with IC50 of 12.21 uM in AlphaScreen assays, limits H2AK119ub1 activity and activates Wnt signaling pathway.
iBP has affinity for PCGF1RAWUL L238A/F242A with a dissociation constant (Kd) of 6.42 uM.
iBP (5-10 uM) is sufficient to inhibit the interaction between PCGF1 and BCOR, without disrupting PRC2 or PRC1.4 integrity.
iBP (10 uM) reduces total H2AK119ub1 levels in 293 T cells, reduces the enrichment of PCGF1, RING1B and H2AK119ub1 levels specifically at target promoter regions.
iBP treatment (20 mg/kg daily, i.p.) enhances OB functions and reverses bone loss in OVX models, enhances upregulation in the expression of osteogenic marker genes and Wnt/β-catenin target genes, effectively activates Wnt signaling and prevents osteoporosis.
iBP enhances osteogenic functions in mouse models of osteoporosis and acute trauma, promotes new bone formation in vivo.