C29

C29 is an inhibitor of toll-like receptor 2 (TLR2) signaling.¹ It inhibits synthetic and bacterial TLR2 agonist-induced TLR2/1 and TLR2/6 signaling in HEK-293T cells expressing human TLR2 (HEK-TLR2) and THP-1 cells when used at a concentration of 50 µM. C29 also inhibits TLR2/1 signaling in primary murine macrophages without inducing cytotoxicity. It decreases the expression of IL-8 induced by the synthetic bacterial lipopeptide TLR2 agonist Pam₃CSK₄ (Item No. 24126) in HEK-TLR2 cells. C29 (150 µM) inhibits the Pam₃CSK₄-induced interaction between TLR2 and the adapter protein MyD88, blocks MAPK activation, and decreases NF-κB activation and IκBα degradation in THP-1 cells.

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1. Mistry, P., Laird, M.H., Schwarz, R.S., et al. Inhibition of TLR2 signaling by small molecule inhibitors targeting a pocket within the TLR2 TIR domain. Proc. Natl. Acad. Sci. USA 112(17), 5455-5460 (2015).