RelB inhibitor RS47 is a potent and specific small molecule targeting RelB (MST, binding Kd=1.1 uM) to inhibit non-canonical NF-κB signaling pathway, with no inhibitory effect on canonical NF-κB signaling pathway.
RS47 inhibitsHCT116 cell viability with IC50 of 1.28 uM, also significantly suppresses the viability of colorectal cancer cell lines (RKO) and breast cancer cell line (MDA-MB-231).
RS47 blocks non-canonical NF-κB signaling pathway through interacting with RelB, RS47 could pull down endogenous RelB protein in HCT116 cells directly, but not NIK and p100.
RS47 interrupts RelB binding to its target DNA, thus inhibiting expression of genes induced by BAFFactivated non-canonical NF-κB signaling pathway.
RS47 represses BAFF-induced survival of primary B lymphoma cells significantly.
RS47 suppresses human colorectal cancer (CRC) cells proliferation and promote cells apoptosis, promotes human B lymphoma cells apoptosis in vitro.
RS47 inhibits tumorigenesis of human B lymphoma from PDX in xenograft model.