STING-IN-19
STING-IN-19 is a STING inhibitor with a Kd value of 2.31 μM for human STING. STING-IN-19 inhibits the activation of TBK1 and IRF3 by binding to STING, thereby suppressing the activation of downstream signaling pathways. STING-IN-19 reduces the levels of key inflammatory cytokines IL-1β, IL-6 and TNF-α in colonic tissues and serum of mice with ulcerative colitis. STING-IN-19 can be used in studies related to ulcerative colitis.
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- Formule: C30H41NO5
- Masse moléculaire:495.65
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Stockage:
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
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Activité biologique
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Chemical Information
- Pureté et documentation
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Activité biologique
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TBK1 |
IL-1β |
IL-6 |
TNF-α |
STING-IN-19 (compound Z55) binds directly to recombinant human STING1 with high affinity, with a Kd value of 2.31 μM; it potently inhibits HT-DNA-induced STING pathway activation in IRF-Luc-THP-1 cells, with an IC50 of 0.40 μM; it exhibits moderate cytotoxicity against IRF-Luc-THP-1 cells, with a cell viability IC50 of 4.75 μM[1].
STING-IN-19 (10 μM; 18 h) directly binds to endogenous STING in RAW264.7 cells, increasing the thermal stability of this protein by 4.31 °C[1].
STING-IN-19 potently inhibits DMXAA-induced activation of the STING pathway in RAW264.7 murine macrophages, and exhibits no cytotoxicity at concentrations up to 3 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAW264.7 cell
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Concentration:10 μM
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Incubation Time:18 h
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Result:Directly engaged endogenous STING in RAW264.7 cells, increasing the protein's thermal stability by 4.31 °C.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, 8 weeks old, 20-22 g, DSS-induced ulcerative colitis)[1]
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Dosage:2, 4 mg/kg
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Administration:i.p.; daily; 7 days
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Result:Significantly attenuated DSS-induced body weight loss.
Reduced Disease Activity Index (DAI) scores.
Alleviated colon shortening, with 4 mg/kg dose showing greater efficacy than 2 mg/kg.
Protected against crypt architecture destruction, reduced inflammatory cell infiltration, and preserved goblet cells (assessed via H&E and PAS staining).
Significantly downregulated protein expression levels of p-STING, p-TBK1, and p-IRF3 in colon tissues at 4 mg/kg.
Reduced serum levels of inflammatory cytokines IL-1β, IL-6, and TNF-α.
Downregulated mRNA expression of IL-1β, IL-6, and TNF-α in colonic tissues.
Chemical Information
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Masse moléculaire 495.65
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Formule C30H41NO5
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SMILES
O=C(O[C@@H]1C[C@](CC[C@]2([H])[C@]3([H])CC[C@@]4(C)[C@]2(O5)[C@H]5C[C@@H]4C6=COC(C=C6)=O)([H])[C@]3(C)CC1)[C@H]7NCCCC7
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
STING-IN-19 Related Classifications
HY-187227 Related Classifications
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