STING-IN-16
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2982807-58-7
- 分子式: C25H22ClN3O2
- 分子量:431.91
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
生物活性
STING-IN-16 (Compound 5c) (1 μM, 24 h) inhibits the activation of STING with IC50s of 44 nM (THP1-Blue-ISG cells) and 32 nM (RAW-Lucia-ISG cells)[1]. STING-IN-16 (0.3-3 μM, 3-6 h) inhibits the STING signaling pathway activated by STING activators and markedly increases STING thermal stability in THP1 cells, BMDM cells, MEF cells and RAW264.7 murine macrophage cells[1]. STING-IN-16 (1 μM, 6 h) inhibits the activation of the cGAS-STING axis triggered by Cisplatin (HY-17394)-induced DNA damage, which in turn reduces ROS accumulation and cell apoptosis in HK2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
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).
-
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.
-
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 Line:HK2 cells
-
Concentration:1 μM
-
Incubation Time:6 h
-
Result:Attenuated Cisplatin-induced cell death.
MedChemExpress (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.
化学情報
-
CAS 番号 2982807-58-7
-
分子量 431.91
-
分子式 C25H22ClN3O2
-
SMILES
O=C(N1CCC2=C(C1)C=CC(C3=CC=C(C=C3)OC)=C2)NC4=CNC5=C4C=C(C=C5)Cl
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
STING-IN-16 関連分類
HY-175210 関連分類
Powered by Bioz