CU-CPT-9a

  Cat. No.:  DC10770   Featured
Chemical Structure
2165340-32-7
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Field of application
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.
Cas No.: 2165340-32-7
Chemical Name: 4-(7-methoxyquinolin-4-yl)-2-methylphenol
SMILES: C(C1=CC=NC2C=C(OC)C=CC1=2)1=CC=C(O)C(C)=C1
Formula: C17H15NO2
M.Wt: 265.31
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: CU-CPT-9a is a specific TLR8 antagonist, with an IC50 of 0.5 nM.
Target: TLR8:0.5 nM (IC50)
In Vitro: CU-CPT-9a is a specific TLR8 antagonist, with an IC50 of 0.5±0.1 nM. The elevation of the downstream protein levels induced by R848 can be reversed by CU-CPT-9a in a dose-dependent manner. By contrast, the expression of TRIF and IRF3 (cytoplasmic and nuclear) are only responsive to TLR4 and TLR3, independent of TLR837. The expression levels of TRIF and IRF3 do not show significant change in THP-1 cells upon treatment of R848, nor do they change with the treatment of CU-CPT-9a. CU-CPT8m and CU-CPT-9a both significantly suppress the TNF-α level in a dose-dependent manner, which is in agreement with previous reports of TLR8 involvement in these autoimmune diseases[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.
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.
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