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CU-115

  Cat. No.:  DC42507   Featured
Chemical Structure
2471982-20-2
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More than 5000 active chemicals with high quality for research!
Field of application
CU115 is a potent TLR8 antagonist (IC50=1.04 µM), and shows selective for TLR8 over TLR7 (IC50=>50 µM). CU 115 decreases TNF-α and IL-1β production activated by R-848 in THP-1 cells.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2471982-20-2
Synonyms: CU-115
SMILES: O=C(NC1=CC=C(OC2=CC(C(F)(F)F)=CC(C(F)(F)F)=C2)C=C1)C3=C(I)C=CC=C3F
Formula: C21H11F7InO2
M.Wt: 569.21
Purity: >98%
Sotrage: Please store the product under the recommended conditions in the Certificate of Analysis.
Publication: [1]. Rosaura Padilla-Salinas, et al. Discovery of Novel Small Molecule Dual Inhibitors Targeting Toll-Like Receptors 7 and 8. J Med Chem. 2019 Nov 27;62(22):10221-10244.
Target: TLR8:1.04 μM (IC50) TLR7:50 μM (IC50)
In Vitro: In endosomal and non-endosomal TLR specificity studies, Human embryonic kidney (HEK) 293 cells expressing human tolllike receptor (hTLR) gene and an inducible secreted embryonic alkaline phosphatase (SEAP) reporter gene were incubated with CU-115 for 16 hours. As a result, CU-115 displays activity for TLR7 and TLR8 at low concentrations (0.5 μM). CU-115 does not modulate the NF-kB inhibition induced by Pam2CSK4, Pam3CSK4, Poly(I:C), LPS, R848, and Flic in HEK-293 TLR1/2, TLR2/6, TLR3, and TLR4 cells. And CU-115 inhibits TLR9 signaling at 1, 5, and 20 µM and ~10-25% inhibition. CU-115 (5-20 µM) inhibits increases in type I IFN transcriptional activity induced by the ssRNA nucleic acid ligands 3p-hpRNA or G3-YSD in a luciferase reporter assay. CU-115 (0.5, 1.0, 5, and 20 µM; 16 hours) is nontoxic at low concentrations (0.5 and 20 μM) and toxic at 100 μM in Hek293 TLR7 and TLR8 cells. CU-115 also is nontoxic at low concentrations (0.5 and 20 μM) and displays partial toxicity at 100 μM in THP Dual cells. The enzyme-linked immunosorbent assay (ELISA) is performed to measure upregulation/inhibition of TNF-α in human THP-1 cells (hTHP-1). CU-115 (5-20 µM) abolishes the TNF-α production activated by R848 (1 µg/ml) in hTHP1. It also represses the expression of IL-1β in hTHP-1 cells. These results suggest that CU-115 suppresses TLR8 and TLR7 signaling pathways.
References: [1]. Rosaura Padilla-Salinas, et al. Discovery of Novel Small Molecule Dual Inhibitors Targeting Toll-Like Receptors 7 and 8. J Med Chem. 2019 Nov 27;62(22):10221-10244.
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