CU-CPT-9a
Names
Biological Activity
[Description]:
CU-CPT-9b is a specific TLR8 antagonist, with an IC50 of 0.7 nM.
[Related Catalog]:
[Target]
TLR8:0.7 nM (IC50)
[In Vitro]
CU-CPT-9b is a specific TLR8 antagonist, with an IC50 of 0.7±0.2 nM. ITC experiments have confirmed the strong binding of CU-CPT-9b with a Kd of 21 nM. It is shown that CU-CPT-9b binds to the inactive TLR8 dimer in a similar way to CU-CPT8m. CU-CPT9b utilizes hydrogen bonds with G351 and V520*, which are conserved among TLR8/antagonist structures. Additionally, CU-CPT-9b forms water-mediated contacts with S516* and Q519*, which are not observed in TLR8/CU-CPT8m structure, suggesting that the enhanced potency of CU-CPT-9b derives from the new interactions with these polar residues. The orientation of Y567* also changes to facilitate van der Waals interactions with CU-CPT-9b as compared to TLR8/CU-CPT8m[1].
[References]
[Related Small Molecules]
Chemical & Physical Properties
[ Molecular Formula ]:
C16H13NO2
[ Molecular Weight ]:
251.28
[ Storage condition ]:
2-8℃