CU-CPT22 is the first probe for the complex between toll-like receptors TLR1 and TLR2. CU-CPT22 binds at the interface of TLR1 and TLR2 (IC50 = 0.58 μM). It competes with the synthetic triacylated lipoprotein (Pam3CSK4) binding to TLR1/2 (Ki: 0.41 μM).

TLR2/1:(ki)0.41 μM

A novel compound (CU-CPT22) that can compete with the synthetic triacylated lipoprotein (Pam3CSK4) binding to TLR1/2 with high inhibitory activity and specificity.CU-CPT22 is a toll-like inhibitor of receptor 1 and 2 (TLR1/2) ( IC50: 0.58±0.09 μM).?CU-CPT22 is found to have no significant cytotoxicity at various concentrations up to 100 μM in RAW 264.7 cells.?It is showed that CU-CPT22 is able to compete with Pam3CSK4 for binding to TLR1/2 (Ki: 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.??The result shows that CU-CPT22 can inhibit about 60% of TNF-αand 95% of IL-1β at 8 μM[1].