CU-CPT9b

SKU: orb1220516

Description

CU-CPT9b is an antagonist of toll-like receptor 8 (TLR8; Kd = 21 nM). It inhibits activation of NF- B induced by the TLR8 agonist R-848 in TLR8-overexpressing HEK-Blue cells with an IC50 value of 0.7 nM.

Key Properties

• CAS Number: 2162962-69-6
• MW: 251.28
• Purity: >98% (HPLC)
• Formula: C₁₆H₁₃NO₂
• SMILES: Cc1cc(ccc1O)-c1ccnc2cc(O)ccc12
• Target: TLR
• Solubility: DMSO:100 mg/mL (397.96 mM)

Bioactivity

• In Vitro:
  CU-CPT9b is a specific TLR8 antagonist, with an IC50 of 0.7±0.2 nM. ITC experiments have confirmed the strong binding of CU-CPT9b 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-CPT9b forms water-mediated contacts with S516* and Q519*, which are not observed in TLR8/CU-CPT8m structure, suggesting that the enhanced potency of CU-CPT9b derives from the new interactions with these polar residues. The orientation of Y567* also changes to facilitate van der Waals interactions with CU-CPT9b as compared to TLR8/CU-CPT8m.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CU-CPT-9b | TLR8-specific antagonist 1

Quick Database Links

Gene Symbol

TLR