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The protein complex of toll-like receptor 1 and 2 (TLR1/2) is an important regulator of innate immunity, and therefore provides an attractive target for the treatment of various immune disordres. Here we report a novel compound (CU-CPT22) that can compete with the synthetic triacylated lipoprotein (Pam 3 CSK 4) binding to TLR1/2 with high inhibitory activity and specificity. Repression of downstream signaling from TNF-α and IL-1β has also been observed.