CU-T12-9

CU-T12-9 is a specific TLR1/2 agonist with EC₅₀ of 52.9 nM in HEK-Blue hTLR2 SEAP assay. CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 selectively activates the TLR1/2 heterodimer, not TLR2/6. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS^[1]. In Vitro: CU-T12-9 directly targets TLR1/2 to initiate downstream signaling. By binding to both TLR1 and TLR2, CU-T12-9 facilitates the TLR1/2 heterodimeric complex formation, which in turn activates the downstream signaling^[1].
CU-T12-9 activates the TLR1/2 pathway by inducing NF-κB activation to trigger downstream signaling, such as secreted embryonic alkaline phosphatase (SEAP), NO, and TNF-α^[1].
CU-T12-9 (0.39-100 μM; 24 hours) does not produce toxicity up to 100 μM in HEK-Blue hTLR2 and Raw 264.7 cells^[1].
CU-T12-9 up-regulates the mRNA levels of TLR1, TLR2, TNF, IL-10, and iNOS. CU-T12-9 (0.1-10 μM) activates TLR1 mRNA and iNOS mRNA after Raw 264.7 cells are treated for 24 hours. CU-T12-9 (0.1-10 μM) activates TLR2 and IL-10 mRNA after Raw 264.7 cells are treated for 2 hours. CU-T12-9 (0.1-10 μM) activates TNF mRNA after Raw 264.7 cells are treated for 8 hours^[1].