CU-CPT9a (TLR8 inhibitor 9a) is a potent, selective TLR8 inhibitor with IC50 of 0.5 nM, and negligible cytotoxicity.
CU-CPT9a shows no significant inhibition for other TLRs at 1 uM in cellular assays.
CU-CPT9a consistently recognizes an allosteric pocket on the protein-protein interface, stabilizing the inactive TLR8 dimer.
CU-CPT9a shows significant inhibitory effects in suppressing the spontaneous release of TNF-α and IL-1β from synovial membrane cultures with little cytotoxicity up to 100 uM, also reduces the cytokine elevation in PMBCs derived from four patients with RA.
Physicochemical Properties
M.Wt
265.312
Formula
C17H15NO2
Appearance
Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
4-(7-methoxyquinolin-4-yl)-2-methylphenol
References
1. Zhang S, et al. Nat Chem Biol. 2017 Nov 20. doi: 10.1038/nchembio.2518.
