2. Immunology/Inflammation NF-κB
  3. Cyclic GMP-AMP Synthase IKK IFNAR
  4. XL-3158

XL-3158是一种口服有效的环鸟苷酸-腺苷酸合成酶 (cGAS) 抑制剂 (人源 cGAS IC50 = 11.1 μM, 鼠源 cGAS IC50 = 2.19 μM)。XL-3158同时占据变构位点和正构位点，使激活环稳定在闭合的非活性构象中，从而减弱 cGAS 与 DNA 的相互作用。XL-3158通过靶向相分离抑制 cGAS。XL-3158通过抑制凝聚体形成高效穿透细胞，有效降低细胞内 cGAS 局部浓度。XL-3158 在有效浓度范围内无明显细胞毒性，适合后续细胞功能实验。XL-3158克服物种选择性障碍，为 cGAS 依赖的炎症性疾病提供候选药物[1]。

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XL-3158 Chemical Structure

XL-3158 Chemical Structure

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XL-3158 相关抗体

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IKK-α IKK-β IKK IKKε TBK1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

XL-3158 is a selective and cross-species Cyclic GMP-AMP synthase (cGAS) inhibitor (IC50: 11.1 μM for human cGAS, 2.19 μM for mouse cGAS). XL-3158 simultaneously occupy allosteric and orthosteric sites, stabilizing the activation loop in a closed, inactive conformation and thereby attenuating the cGAS-DNA interactions. XL-3158 inhibits cGAS by targeting phase separation. XL-3158 efficiently penetrates cells by inhibiting aggregate formation, effectively reducing the local concentration of cGAS within cells. XL-3158 has no obvious cytotoxicity within the effective concentration range and is suitable for subsequent cell function experiments. XL-3158 overcomes species selectivity barriers and serves as a drug candidate for cGAS-dependent inflammatory diseases[1].

体外研究
(In Vitro)

XL-3158 (Compound XL-3158) (20 μM, 4 h) 通过抑制 L929 细胞中 cGAS 相分离，阻断 cGAS 与 DNA 的细胞內凝聚[1]。

XL-3158 (10-40 μM, 4 h) 在 THP-1 Dual 细胞中特异性抑制 cGAS-STING 通路下游信号激活[1]。

XL-3158 (10 μM, 4 h) 在 THP-1 Dual 细胞中选择性抑制 DNA 触发的 cGAS 依赖性干扰素通路[1]。

XL-3158 (0-20 μM, 24 h) 对 THP-1 细胞的 CC50 为 77.55 μM，对 RAW-ISG 细胞的 CC50 为 56.79 μM[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

XL-3158 相关抗体:

Western Blot Analysis[1]

Cell Line: THP-1 Dual cells
Concentration: 10 μM, 20 μM, 40μM
Incubation Time: 4 h
Result: Inhibited HT-DNA-induced TBK-1 and IRF3 phosphorylation in a dose-dependent manner.
Had no inhibitory effect on pathways activated by Poly (I:C) or cGAMP.

RT-PCR[1]

Cell Line: THP-1 Dual cells
Concentration: 10 μM, 20 μM, 40μM
Incubation Time: 4 h
Result: Significantly reduced HT-DNA-induced IFN-β1 mRNA expression.

Immunofluorescence[1]

Cell Line: L929 cells
Concentration: 20 μM
Incubation Time: 4 h
Result: Significantly reduced the number of co-localized condensates of cGAS and Cy5-DNA.
Confirmed that the condensates had liquid-like properties (LLPS) and inhibited their formation.
体内研究
(In Vivo)

XL-3158 (Compound XL-3158) (25 mg/kg, i.g. 两次给药) 对急性胰腺炎有显著缓解作用，具有良好的口服生物利用度和体内活性，支持其作为 cGAS 依赖性炎症疾病的候选药物[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Cerulean (HY-A0190) (50 µg/kg, i.p, injections once every hour for 7 times) induced acute pancreatitis model in C57BL/6J nude female mice (6-8 weeks)[1].
Dosage: 25mg/kg
Administration: Intragastric gavage (i.g.), administration at 0 hour and 6 h after the first Cerulein injection.
Result: Significantly reduced pancreatic pathological damage and the pancreas/body weight ratio, indicating that pancreatic edema was relieved.
Significantly reduced serum amylase and serum lipase activities.
Significantly reduced serum inflammatory factor levels.
分子量

690.61

Formula

C30H17F7N6O2S2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

XL-3158 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

XL-3158XL3158XL 3158Cyclic GMP-AMP SynthaseIKKIFNARcGASIκB kinaseI kappa B kinase Interferon-α/β receptorInterferon-alpha/beta receptorAcute Pancreatitis modelC57BL/6J miceICR miceAllosteric inhibitorOral bioavailabilityTHP-1 Dual cellsInhibitorinhibitorinhibit

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