CU-CPT9b is an antagonist of toll-like receptor 8 (TLR8; Kd = 21 nM). It inhibits activation of NF-ĸB induced by the TLR8 agonist R-848 in TLR8-overexpressing HEK-Blue cells with an IC50 value of 0.7 nM.
CU-CPT9a is a potent TLR8 inhibitor (IC50 = 0.5 nM and Kd = 21 nM). Stabilizes the TLR8 dimer in its resting state, preventing activation. Suppresses TLR8-mediated proinflammatory signaling in various cell lines and human primary cells.
TLR8: 0.7 nM (IC50); TLR8: 21 nM (Kd)
[1] SHUTING ZHANG. Small-molecule inhibition of TLR8 through stabilization of its resting state[J]. Nature chemical biology, 2017, 14 1: 58-64. DOI:
10.1038/nchembio.2518
