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

XL-3158 Chemical Structure

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规格 价格 是否有货 数量
5 mg ￥1330
In-stock
10 mg ￥2150
In-stock
25 mg ￥4300
In-stock
50 mg 现货 询价
100 mg 现货 询价
200 mg 现货 询价
500 mg   询价  
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Customer Review

XL-3158 相关抗体

Top Publications Citing Use of Products

查看 IKK 亚型特异性产品:

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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
性状

固体

颜色

Off-white to light yellow

运输条件

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

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 50 mg/mL (72.40 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.4480 mL 7.2400 mL 14.4800 mL
5 mM 0.2896 mL 1.4480 mL 2.8960 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-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。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

XL-3158 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.4480 mL 7.2400 mL 14.4800 mL 36.1999 mL
5 mM 0.2896 mL 1.4480 mL 2.8960 mL 7.2400 mL
10 mM 0.1448 mL 0.7240 mL 1.4480 mL 3.6200 mL
15 mM 0.0965 mL 0.4827 mL 0.9653 mL 2.4133 mL
20 mM 0.0724 mL 0.3620 mL 0.7240 mL 1.8100 mL
25 mM 0.0579 mL 0.2896 mL 0.5792 mL 1.4480 mL
30 mM 0.0483 mL 0.2413 mL 0.4827 mL 1.2067 mL
40 mM 0.0362 mL 0.1810 mL 0.3620 mL 0.9050 mL
50 mM 0.0290 mL 0.1448 mL 0.2896 mL 0.7240 mL
60 mM 0.0241 mL 0.1207 mL 0.2413 mL 0.6033 mL
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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