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CU-CPT-9a

Names

[ CAS No. ]:
2162962-69-6

[ Name ]:
CU-CPT-9a

[Synonym ]:
CPD1577

Biological Activity

[Description]:

CU-CPT-9b is a specific TLR8 antagonist, with an IC50 of 0.7 nM.

[Related Catalog]:

Signaling Pathways >> Immunology/Inflammation >> Toll-like Receptor (TLR)
Research Areas >> Inflammation/Immunology

[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]

[1]. Zhang S, et al. Small-molecule inhibition of TLR8 through stabilization of its resting state. Nat Chem Biol. 2018 Jan;14(1):58-64.


[Related Small Molecules]

TAK-242 | Chloroquine diphosphate | Resiquimod | TLR2-IN-C29 | imiquimod | Hydroxychloroquine sulfate | GS-9620 | Motolimod | CU CPT 22 | Atractylenolide I | E6446 dihydrochloride | CU-CPT17e | Paquinimod | Gardiquimod trifluoroacetate | Procyanidin B1

Chemical & Physical Properties

[ Molecular Formula ]:
C16H13NO2

[ Molecular Weight ]:
251.28

[ Storage condition ]:
2-8℃


Related Compounds