CU-115

Research use only, not for human use.

CU-115 is a selective antagonist of TLR8 with IC50s of 1.04 μM and >50 μM for TLR8 and TLR7, respectively.

CU-115 is a selective antagonist of TLR8 with IC50s of 1.04 μM and >50 μM for TLR8 and TLR7, respectively.(In Vitro):CU-115 (1, 5, and 20 μM) inhibits TLR9 to 10-25% inhibition. CU-115 (5-20 μM) inhibits increases in the activity of type I IFN transcriptional induced by the ssRNA nucleic acid ligands 3p-hpRNA or G3-YSD. CU-115 (5-20 μM) abolishes the TNF-α production activated by R848 (1 μg/ml) and represses the expression of IL-1β in hTHP-1 cells. CU-115 does not modulate the NF-kB inhibition induced by Pam2CSK4, Pam3CSK4, LPS, R848, Poly(I:C), and Flic in HEK-293 TLR1/2, TLR2/6, TLR3, and TLR4 cells.

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.

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N-(4-(3,5-bis(trifluoromethyl)phenoxy)phenyl)-2-fluoro-6-iodobenzamide

Immunology/Inflammation

TLR

ABHD6

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2471982-20-2

569.21

C21H11F7INO2

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (175.68 mM)

O=C(NC1=CC=C(OC=2C=C(C=C(C2)C(F)(F)F)C(F)(F)F)C=C1)C=3C(F)=CC=CC3I

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(-20℃)

With Ice Pack

≥ 2 years