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ChX710是一种小分子化合物,能够启动I型干扰素对胞质DNA的反应。

ChX710 Chemical Structure

Cas No.:2438721-44-7

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥741.00
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1mg
¥398.00
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5mg
¥1,042.00
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10mg
¥1,567.00
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25mg
¥2,599.00
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50mg
¥3,614.00
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Sample solution is provided at 25 µL, 10mM.

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Description

ChX710 is a small-molecule compound that primes the type I interferon response to cytosolic DNA. ChX710 induces the interferon-stimulated response element (ISRE) promoter, specific interferon-stimulated genes (ISGs), and phosphorylation of interferon regulatory factor (IRF)3, effectively priming the cellular response to DNA transfection via the STING pathway[1].

In vitro, ChX710 (6–50μM) was applied to cell lines such as HEK-293 for 8–48 hours. ChX710 specifically activates the ISRE promoter and induces phosphorylation of IRF3. ChX710 effectively enhances the cellular type I interferon response to cytosolic (transfected) DNA, leading to increased IFN-β secretion. At higher concentrations (25–50µM), ChX710 exhibits significant cytotoxicity, reducing cellular ATP levels and viability[1].

References:
[1] Khiar S, Lucas-Hourani M, Nisole 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.

ChX710是一种小分子化合物,能够启动I型干扰素对胞质DNA的反应。ChX710可诱导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,通过STING途径有效启动细胞对DNA转染的反应[1]

在体外,ChX710(6–50μM)处理HEK-293等细胞系8-48小时。ChX710特异性激活ISRE启动子,可诱导IRF3的磷酸化。ChX710可有效增强细胞对胞质(转染)DNA的I型干扰素反应,导致IFN-β分泌。ChX710在高浓度(25-50µM)下表现出显著的细胞毒性,降低细胞ATP水平和活力[1]

实验参考方法

Cell experiment [1]:

Cell lines

HEK-293T (human embryonic kidney epithelial cells), A549 (human lung epithelial adenocarcinoma cells), MRC5 (human lung fibroblasts), Vero (African green monkey kidney epithelial cells), and primary human peripheral blood mononuclear cells (PBMCs)

Preparation Method

Reporter cell lines (e.g., STING-37, a HEK-293 cell line stably expressing luciferase under the control of ISRE) or other cell types were cultured in Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% fetal calf serum (FCS), penicillin, and streptomycin at 37°C and 5% CO₂. Cells were treated with ChX710 (6-50µM) or related compounds for specified durations. For synergy experiments, cells were co-treated with ChX710 and transfected with plasmid DNA or stimulated with 2',3'-cGAMP using JetPrime transfection reagent.

Reaction Conditions

6-50µM; 8-48 hours.

Applications

ChX710 specifically activates the Interferon-Stimulated Response Element (ISRE) promoter. This activation is dependent on the adaptor protein MAVS and the transcription factor IRF1, but independent of STAT1/STAT2. ChX710 induces phosphorylation of IRF3 but is insufficient to trigger type I interferon (IFN-α/β) secretion on its own. ChX710 induces a modest, cell-type-specific profile of Interferon-Stimulated Genes (ISGs). Crucially, ChX710 potently primes and synergistically enhances the cellular type I interferon response to cytosolic (transfected) DNA, leading to a strong, STING-dependent increase in IFN-β secretion and ISG expression. ChX710 exhibits significant cytotoxicity at higher concentrations, reducing cellular ATP levels and viability.

References:
[1] Khiar S, Lucas-Hourani M, Nisole 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.

化学性质

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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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mg 5 mg 10 mg
1 mM 3.0922 mL 15.4612 mL 30.9224 mL
5 mM 618.4 μL 3.0922 mL 6.1845 mL
10 mM 309.2 μL 1.5461 mL 3.0922 mL
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