CU-CPT-9b|cas 2162962-69-6|TLR8 inhibitor

Cas No.:	2162962-69-6
Chemical Name:	4-(4-hydroxy-3-methylphenyl)quinolin-7-o
SMILES:	OC1C=CC2C(=CC=NC=2C=1)C1C=C(C)C(O)=CC=1
Formula:	C₁₆H₁₃NO₂
M.Wt:	251.28
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

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

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].

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101

Cat. No.	Product name	Field of application
DC70332	CU-CPD107	CU-CPD107 is a TLR8-specific small molecule with unique synergistic agonist activities in the presence of ssRNA, but inactive without the aid of ssRNA.CU-CPD107 significantly inhibited of R848-induced signaling in HEK-Blue hTLR8 cells with an IC50 of 13.7 uM.CU-CPD107 only inhibited synthesized small-molecule agonist-induced TLR8 signaling without affecting other TLRs.CU-CPD107 synergistically increased IFN-β, TNF-α, IL-1β, IL-6, and IL-8 mRNA expression levels in the presence of 5 μg/ml ssRNA40 in HEK-Blue hTLR8 cells, whereas CU-CPD107 alone did not. CU-CPD107 only activated TLR8-mediated signaling in the presence of ssRNA.CU-CPD107 showed no pure agonistic activity, addressing a major challenge that has existed for previous TLR7 and TLR8 agonists as vaccine adjuvants or antiviral drugs.
DC10770	CU-CPT-9a	CU-CPT9a is an antagonist of toll-like receptor 8 (TLR8). It inhibits activation of NF-κB induced by the TLR8 agonist R-848 in TLR8-overexpressing HEK-Blue cells (IC50 = 0.5 nM). CU-CPT9a reverses R-848-induced increases in NF-κB p65, IRAK-4, and TRAF3 protein levels in HEK-Blue cells.
DC10769	CU-CPT-9b	CU-CPT9b is an antagonist of toll-like receptor 8 (TLR8; Kd = 21 nM).
DC10771	CU-CPT-8m	CU-CPT-8m is a nolve TLR8 inhibitor.
DC10276	C29	C29 is a potential TLR2 inhibitor.