DRI-C21045 is a novel small-molecule inhibitor of CD40-CD40L protein-protein interaction with IC50 of 0.17 uM in cell-based assays.
DRI-C21045 shows >100-fold selectivity in the ability to inhibit the CD40 vs the TNF interaction.
DRI-C21045 demonstrates concentrationdependent inhibition of CD40L-induced activation of NF-κB in cells with IC50 of 17.1 uM, also inhibits CD40L-induced marker expression in THP cells and B cell activation.
DRI-C21045 inhibits alloantigen-induced immune response in mice model (20-60 mg/kg; s.c.; b.i.d.).
