2. Immunology/Inflammation
  3. STING
  4. STING-IN-8

STING-IN-8 (Compound 15b) 是一种有效的干扰素基因刺激因子 (STING) 抑制剂，对人的 IC50 值为 0.121 μM，小鼠的IC50 值为 0.033 μM。STING-IN-8 抑制 MSA -2 (HY-136927) 或 2’, 3’ -cGAMP (HY-100564) 刺激 STING 信号传导和人、小鼠细胞中的免疫炎症细胞因子水平。 STING-IN-8 在 STING 相关炎症和自身免疫性疾病领域的研究前景广阔。

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STING-IN-8 Chemical Structure

STING-IN-8 Chemical Structure

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STING-IN-8 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

STING-IN-8 (Compound 15b) emerges as a potent stimulator of interferon gene (STING) inhibitor with an IC50 value of 0.121 μM in human and an IC50 value of 0.033 μM in mouse. STING-IN-8 inhibits MSA-2 (HY-136927) or 2’, 3’ -cGAMP (HY-100564)-stimulated STING signaling and suppresses immune-inflammatory cytokine levels in both human and murine cells. STING-IN-8 is promising for research in the field of STING-associated inflammatory and autoimmune diseases[1].
体外研究
(In Vitro)

STING-IN-8 (0.1, 0.3, 1, 3 μM, 5 h) 抑制人和鼠细胞中 MSA-2 (10 μM) 或 2’, 3’ -cGAMP (10 μM) 诱导的 p-TBK1 和 p-IRF3 上调表达[1]。
STING-IN-8 在 THP1-Dual 和 RAW-Lucia 细胞系中 CC50 为 30 μM 时显示出可忽略的细胞毒性[1]。
STING-IN-8 (0.3, 1, 3 μM 和 0.1, 1, 3 μM, 9 h) 在人和小鼠免疫细胞中有效抑制 STING 下游免疫炎症细胞因子[1]。

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

STING-IN-8 相关抗体:

Western Blot Analysis[1]

Cell Line: Human monocyte derived THP1-Dual cell line, murine macrophage cells and mouse embryonic fibroblasts
Concentration: 0.1, 0.3, 1, 3 μM
Incubation Time: 5 h
Result: Significantly down-regulate the the levels of phosphorylated TBK1 and IRF3 induced by MSA-2 (10 μM) and 2’, 3’ -cGAMP (10 μM) in all cell lines with better potency than SN-011 (HY-145010).

Real Time qPCR[1]

Cell Line: THP1-Dual cell line and RAW-Lucia cells
Concentration: 0.3, 1, 3 μM and 0.1, 1, 3 μM
Incubation Time: 9 h
Result: Significantly inhibited the MSA-2 (10 μM) or 2’, 3’-cGAMP (10 μM)-induced upregulation of STING signals expression in THP1-Dual cell line and RAW-Lucia cells.
体内研究
(In Vivo)


STING-IN-8在小鼠体内的药动学参数[1]

药代动力学分析[1]

Administration T1/2 (h) Tmax(h) Cmax(ng/mL) AUC0-∞ (ng·h/mL) MRT(h)
p.o. 10 mg/ kg b 1.75 0.25 77.6 109 2.53
i.p. 5 mg/kgc 4.86 0.18 137 100 4.73

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

Animal Model: C57BL/6 mice
Dosage: 10 MG/KG
Administration: i.p., a single dose
Result: Effectively reduced MSA-2 (10 MG/KG) -stimulated serum IL-6, CXCL10 levels and inhibited the expression of IFNβ, TNFα, ISG15, ISG56, Cxcl10, IL6 in kidney tissues[1]
Animal Model: Kidney tissues of Trex1-D18N mice
Dosage: 10 MG/KG
Administration: i.p. daily for two weeks
Result: Significantly reduced the ISG 15, ISG 56, CXCL10 levels in kidney and demonstrated anti-inflammatory effects in tongue and other muscle tissues of Trex1-D18N mice[1]
分子量

473.45

Formula

C18H14F3N3O5S2
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

STING-IN-8 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 *
= × ×

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)
× = ×
C1   V1   C2   V2
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:

STING-IN-8STINGStimulator of Interferon GenesTMEM173MITAERISMPYSSTING-associated inflammatory and autoimmune diseasesTrex1-D18N miceTHP1-Dual cellRAW-Lucia cellInhibitorinhibitorinhibit

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目录号：
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