2471982-20-2
2471982-20-2 structure
- Name: CU-115
- Chemical Name: CU-115
- CAS Number: 2471982-20-2
- Molecular Formula: C21H11F7INO2
- Molecular Weight: 569.211
- Catalog: Signaling Pathways Immunology/Inflammation Toll-like Receptor (TLR)
- Create Date: 2021-07-28 09:15:51
- Modify Date: 2024-02-23 18:39:04
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CU-115 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[1].
| Name | CU-115 |
|---|---|
| Synonyms |
Benzamide, N-[4-[3,5-bis(trifluoromethyl)phenoxy]phenyl]-2-fluoro-6-iodo-
N-{4-[3,5-Bis(trifluoromethyl)phenoxy]phenyl}-2-fluoro-6-iodobenzamide CU-115 |
| Description | CU-115 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[1]. |
|---|---|
| Related Catalog | |
| 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 |
| Density | 1.7±0.1 g/cm3 |
|---|---|
| Boiling Point | 427.3±45.0 °C at 760 mmHg |
| Molecular Formula | C21H11F7INO2 |
| Molecular Weight | 569.211 |
| Flash Point | 212.2±28.7 °C |
| Exact Mass | 568.972290 |
| LogP | 5.16 |
| Vapour Pressure | 0.0±1.0 mmHg at 25°C |
| Index of Refraction | 1.577 |