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Dri-c21045 showed concentration-dependent inhibition of NF-kB activation and all CD40L induced by B cell proliferation with IC50 of 17.1 μM and 4.5 μM, respectively. Dri-c21045 is an effective selective inhibitor of CD40-CD40L synergistic stimulator protein-protein interaction (PPI) with IC50 of 0.17 μM.