Description
CSLP43 (RIPK2 inhibitor CSLP43) is a novel potent, ATP pocket-binding RIPK2 inhibitor with IC50 of 19.9nM in ADPGlo assay, demonstrates inhibition of both the RIPK2-XIAP interaction, and of cellular and in vivo NOD2 signaling; exhibits inhibition of TNF release from RAW264.7 cells with EC50 of 1.2nM, inhibits NF-kappaB reporter activity with IC50 of 1.34nM; antagonizes NOD2 signaling by interfering with the XIAP-RIPK2 interaction, selectively inhibits NOD responses in cells (HEKBlue NOD2 IC50=1.3nM) and displays potent activity in vivo, does not attenuates the TNF release following an unrelated pro-inflammatory stimulation mediated through TLR4 activation by LPS at 1uM