DRI-C21045

DRI-C21045 (compound 10) is a potent and selective inhibitor of the CD40-CD40L costimulatory protein-protein interaction (PPI) with an IC₅₀ of 0.17 µM. DRI-C21045 shows concentration-dependent inhibition of the activation of NF-κB and B cell proliferation all induced by CD40L with IC₅₀s of 17.1 µM and 4.5 µM, respectively^[1]. IC50 & Target:IC50: 0.17 µM (CD40)^[1] In Vitro:DRI-C21045 (3.2-100 μM; 18 h) concentration-dependently inhibits the CD40L-induced NF-κB activation in CD40 sensor cells^[1].
DRI-C21045 (0.6-50 μM; 48 h) blocks CD40L-induced functional activation of primary B cells^[1].
DRI-C21045 (0.4-50 μM; 48 h) inhibits CD40L-induced MHC-II upregulation in THP-1 cells^[1].
DRI-C21045 (2-100 μM; 48 h) inhibits CD40L-induced B cell proliferation^[1].
DRI-C21045 shows no signs of cytotoxicity for concentrations of up to 100 and 200 µM and has no genotoxic potential for concentrations of up to 500 µM^[1]. In Vivo:DRI-C21045 (30 mg/kg; daily, s.c.; in 20% HPβCD) prolongs graft survival in a murine allogeneic skin transplant model^[1].
DRI-C21045 (20-60 mg/kg; twice daily s.c.; in 20% HPβCD) inhibits alloantigen-induced T cell expansion in the draining lymph nodes (DLNs)^[1].