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CU-CPT22 is a potent protein complex of toll-like receptor 1 and 2 (TLR1/2) inhibitor, and competes with the synthetic triacylated lipoprotein (Pam3CSK4) binding to TLR1/2 with a Ki of 0.41 μM. CU-CPT22 blocks Pam3CSK4-induced TLR1/2 activation with an IC50 of 0.58 μM[1].

CU-CPT22 is a toll-like receptor 1 and 2 (TLR1/2) inhibitor with an IC50 of 0.58±0.09 μM. It is demonstrated that CU-CPT22 is able to compete with Pam3CSK4 for binding to TLR1/2 with an inhibition constant (Ki) of 0.41±0.07 μM, which is consistent with its potency observed in the whole cell assay. Increasing the concentration of CU-CPT22 to 6 μM decreases the anisotropy to background levels. It is found that CU-CPT22 inhibits TLR1/2 signaling without affecting other TLRs, showing it is highly selective in intact cells. CU-CPT22 is found to have no significant cytotoxicity at various concentrations up to 100 μM in RAW 264.7 cells. The result demonstrates that CU-CPT22 can inhibit about 60% of TNF-αand 95% of IL-1β at 8 μM[1]..
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