Description: CU-CPT-9a HCl, an analog of CU-CPT-8m, is a potent and specific antagonist of TLR8 (Toll-like receptor 8) with IC50 of 0.5 nM. Endosomal Toll-like receptors (TLR3, TLR7, TLR8, and TLR9) are highly analogous sensors for various viral or bacterial RNA and DNA molecular patterns. Nonetheless, few small molecules can selectively modulate these TLRs. The elevation of the downstream protein levels induced by R848 can be reversed by CU-CPT-9a in a dose-dependent manner. By contrast, the expression of TRIF and IRF3 (cytoplasmic and nuclear) are only responsive to TLR4 and TLR3, independent of TLR837. The expression levels of TRIF and IRF3 do not show significant change in THP-1 cells upon treatment of R848, nor do they change with the treatment of CU-CPT-9a. CU-CPT8m and CU-CPT-9a both significantly suppress the TNF-α level in a dose-dependent manner, which is in agreement with previous reports of TLR8 involvement in these autoimmune diseases.

References: Nat Chem Biol. 2018 Jan;14(1):58-64.

Related CAS#:125079-83-6 (CU-CPT-8m); 2109805-75-4 CU-CPT17e); 2165340-32-7 (CU-CPT-9a); 2162962-69-6 (CU-CPT-9b)

纯度：≥98%