ChX710
目录号 : GC34329ChX710可以启动I型干扰素对胞质DNA的反应,诱导ISRE启动子序列、特异性细胞干扰素刺激基因(ISGs)和干扰素调节因子(IRF)3的磷酸化。
Cas No.:2438721-44-7
Sample solution is provided at 25 µL, 10mM.
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ChX710 could prime the type I interferon response to cytosolic DNA, which induces the ISRE promoter sequence, specific cellular Interferon-Stimulated Genes (ISGs), and the phosphorylation of Interferon Regulatory Factor (IRF) 3.
ChX710 treatment is found to efficiently prime the cellular response to DNA transfection via STING as assessed by strong synergistic effects on IFN-β expression at both transcriptional and protein levels [1].
[1]. Khiar S, et al. Identification of a small molecule that primes the type I interferon response to cytosolic DNA. Sci Rep. 2017 May 31;7(1):2561.
Cas No. | 2438721-44-7 | SDF | |
Canonical SMILES | O=C(NC(C)CN(C)C)C1=C(N=C(C2=CC=NC=C2)N3)C3=CC=C1 | ||
分子式 | C18H21N5O | 分子量 | 323.39 |
溶解度 | DMSO : 20 mg/mL (61.84 mM) | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 3.0922 mL | 15.4612 mL | 30.9224 mL |
5 mM | 0.6184 mL | 3.0922 mL | 6.1845 mL |
10 mM | 0.3092 mL | 1.5461 mL | 3.0922 mL |
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Identification of a small molecule that primes the type I interferon response to cytosolic DNA
Sci Rep 2017 May 31;7(1):2561.PMID:28566766DOI:PMC5451460
The type I interferon response plays a pivotal role in host defense against infectious agents and tumors, and promising therapeutic approaches rely on small molecules designed to boost this system. To identify such compounds, we developed a high-throughput screening assay based on HEK-293 cells expressing luciferase under the control of Interferon-Stimulated Response Elements (ISRE). An original library of 10,000 synthetic compounds was screened, and we identified a series of 1H-benzimidazole-4-carboxamide compounds inducing the ISRE promoter sequence, specific cellular Interferon-Stimulated Genes (ISGs), and the phosphorylation of Interferon Regulatory Factor (IRF) 3. ISRE induction by ChX710, a prototypical member of this chemical series, was dependent on the adaptor MAVS and IRF1, but was IRF3 independent. Although it was unable to trigger type I IFN secretion per se, ChX710 efficiently primed cellular response to transfected plasmid DNA as assessed by potent synergistic effects on IFN-β secretion and ISG expression levels. This cellular response was dependent on STING, a key adaptor involved in the sensing of cytosolic DNA and immune activation by various pathogens, stress signals and tumorigenesis. Our results demonstrate that cellular response to cytosolic DNA can be boosted with a small molecule, and potential applications in antimicrobial and cancer therapies are discussed.