2. Immunology/Inflammation NF-κB Metabolic Enzyme/Protease Apoptosis
  3. STING Interleukin Related IFNAR Reactive Oxygen Species (ROS) Apoptosis
  4. STING-IN-16

STING-IN-16 是一种 STING 抑制剂，其对 STING 抑制的 IC50 值分别为 44 nM (人) 和 32 nM (鼠). STING-IN-16 有效抑制人源细胞和小鼠细胞中 STING 轴的激活。STING-IN-16 能恢复肾脏线粒体功能，抑制活性氧 (ROS) 的生成，并减少细胞凋亡 (apoptosis)。STING-IN-16 显示出显著的体内抗炎效果。 STING-IN-16 可用于自身免疫和自身炎症性疾病的研究。

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STING-IN-16

STING-IN-16 Chemical Structure

CAS No. : 2982807-58-7

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STING-IN-16 相关抗体

Top Publications Citing Use of Products

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

STING-IN-16 is a STING inhibitor with IC50 values of 44 nM (human) and 32 nM (mice) for cellular STING inhibition. STING-IN-16 effectively inhibits the activation of the STING axis in both human and murine cells. STING-IN-16 can restore renal mitochondrial function, suppress reactive oxygen species (ROS) production, and reduce cell apoptosis. STING-IN-16 shows robust anti-inflammatory efiicacy in vivo. STING-IN-16 can be used for the study of autoimmune and autoinflammatory diseases[1].

体外研究
(In Vitro)

STING-IN-16 (Compound 5c) (1 μM, 24 h) 抑制 STING的激活，IC50 分别为 44 nM (THP1-Blue-ISG) 和 32 nM (RAW-Lucia-ISG 细胞)[1]。
STING-IN-16 (0.3-3 μM, 3-6 h) 抑制 THP1 细胞、骨髓来源巨噬细胞 (BMDM)、小鼠胚胎成纤维细胞 (MEF)和小鼠巨噬细胞 (RAW264.7) 中 STING 激动剂诱导的 STING 信号激活并显著提高 STING 的热稳定性[1]。
STING-IN-16 (1 μM, 6 h) 抑制 HK2 细胞中由 Cisplatin (HY-17394) 诱导的 DNA 损伤触发的 cGAS-STING 轴激活，从而减少 ROS 积累和细胞凋亡[1]。

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

STING-IN-16 相关抗体:

Western Blot Analysis[1]

Cell Line: THP1 cells, BMDM cells, HK2 cells
Concentration: 0.3, 1, 3 μM
Incubation Time: 6 h
Result: Inhibited MSA-2 (HY-136927)-stimulated phosphorylation of STING, TBK1, and IRF3, showing better activity than H151(HY-112693) in THP1 cells.
Inhibited Vadimezan (DMXAA) (HY-10964)-stimulated phosphorylation of STING, TBK1, and IRF3, showing better activity than H151 in BMDM cells.
Inhibited cisplatin-stimulated phosphorylation of STING, TBK1, IRF3, and P65, exhibiting higher potency than H151 in HK2 cells.
Decreased the expression of apoptosis markers such as cleaved-caspase3, cleaved-caspase8, and DNA damage markers (γ-H2A.X and p-CHK1).

Real Time qPCR[1]

Cell Line: THP1 cells, BMDM cells, HK2 cells
Concentration: 0.3, 1, 3 μM
Incubation Time: 3, 6 h
Result: Inhibited MSA-2-triggered gene expression of the cytokines (ISG15, ISG56, IFNβ, CXCL10 and CCL5) dose-dependently in THP1 cells.
Inhibited DMXAA-triggered gene expression of the cytokines (ISG15, ISG56, IFNβ, CXCL10 and CCL5) dose-dependently in BMDM cells.
Inhibited diABZI STING agonist-1 (HY-112921A), cGAMP (HY-12512) and HTDNA-triggered gene expression of the cytokines ( IFNβ, IL6, CXCL10 and ISG15) in THP1 cells and BMDM cells.
Reduced cisplatin-induced gene expression of inflammatory cytokines such as IL6, TNFA, IL8 and CXCL10 in HK2 cells.

ELISA Assay[1]

Cell Line: THP1 cells, BMDM cells
Concentration: 0.3, 1, 3 μM
Incubation Time: 6 h
Result: Decreased MSA-2-induced secretion of IFN-β, CXCL10, and IL-6, showing considerably higher potency than H151 in THP1 cells.
Decreased DMXAA-induced secretion of IFN-β, CXCL10, and IL-6, showing considerably higher potency than H151 in BMDM cells.

Cell Viability Assay[1]

Cell Line: HK2 cells
Concentration: 1 μM
Incubation Time: 6 h
Result: Attenuated Cisplatin-induced cell death.
体内研究
(In Vivo)

STING-IN-16 (Compound 5c) (10 mg/kg，腹腔注射，每日一次，持续 3 天) 缓解小鼠中 Cisplatin (顺铂) (HY-17394) 诱导的炎症[1]。
STING-IN-16 (10 mg/kg，腹腔注射，单次剂量) 在 MSA-2 诱导的炎症小鼠模型中显示出抗炎效果[1]。

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

Animal Model: Cisplatin-induced kidney injury C57BL/6 male mice (8 weeks)[1]
Dosage: 10 mg/kg
Administration: i.p. daily for 3 days
Result: Blocked the expression of Ifnb, Il6, and Tnfa.
Reduced cisplatin-induced BUN elevation.
Alleviated cisplatin-induced pathological changes (severe tubular dilation, tubular necrosis, and cast formation).
Reduced cisplatin-induced elevation of plasma IL-6, which was better than that of H151.
Restored the expression of such mitochondria-encoded genes(mt-CO1, mt-CO2, mt-CO3, mt-ATP6, mt-ND2 and mt-ND4).
Animal Model: MSA-2-induced inflammation C57BL/6 male mice (8 weeks)[1]
Dosage: 10 mg/kg
Administration: i.p. for a single dose
Result: Decreased MSA-2-induced cytokines secretion in serum, including IFN-β, CXCL10, and IL-6.
Diminished MSA-2-induced expression of Ifnb and Il6 in the kidney tissue.
Lowered MSA-2-stimulated expression of Ifnb, Il6, and Ccl5 in the heart tissue.
分子量

431.91

Formula

C25H22ClN3O2
CAS 号
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-16 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

STING-IN-162982807-58-7STINGInterleukin RelatedIFNARReactive Oxygen Species (ROS)ApoptosisStimulator of Interferon GenesTMEM173MITAERISMPYSILInterferon-α/β receptorInterferon-alpha/beta receptor THP1 cellsBMDM cellsMEF cellsRAW264.7 cellsROSapoptosisinflammationInhibitorinhibitorinhibit

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