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.
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- CAS No.: 2982807-58-7
- 화학식: C25H22ClN3O2
- 분자량:431.91
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보관:
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]
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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.
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Cell Line:THP1 cells, BMDM cells, HK2 cells
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Concentration:0.3, 1, 3 μM
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Incubation Time:6 h
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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).
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Cell Line:THP1 cells, BMDM cells, HK2 cells
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Concentration:0.3, 1, 3 μM
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Incubation Time:3, 6 h
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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.
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Cell Line:THP1 cells, BMDM cells
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Concentration:0.3, 1, 3 μM
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Incubation Time:6 h
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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.
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Cell Line:HK2 cells
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Concentration:1 μM
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Incubation Time:6 h
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Result:Attenuated Cisplatin-induced cell death.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Cisplatin-induced kidney injury C57BL/6 male mice (8 weeks)[1]
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Dosage:10 mg/kg
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Administration:i.p. daily for 3 days
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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).
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Animal Model:MSA-2-induced inflammation C57BL/6 male mice (8 weeks)[1]
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Dosage:10 mg/kg
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Administration:i.p. for a single dose
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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.
Chemical Information
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CAS No. 2982807-58-7
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분자량 431.91
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화학식 C25H22ClN3O2
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SMILES
O=C(N1CCC2=C(C1)C=CC(C3=CC=C(C=C3)OC)=C2)NC4=CNC5=C4C=C(C=C5)Cl
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
STING-IN-16 Related Classifications
HY-175210 Related Classifications
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