STING-IN-20
STING-IN-20 is an orally active STING inhibitor with a Kd of 0.699 μM. STING-IN-20 binds to the orthosteric binding pocket of STING CTD and inhibits cGAMP-induced STING activation, oligomerization, and downstream TBK1/IRF3 phosphorylation. STING-IN-20 inhibits NLRP3-related pyroptosis and IL-1β expression, restores autophagic flux and phagocytic capacity, attenuates mitochondrial depolarization, and reduces macrophage-to-β cell mitochondrial transfer in macrophages. STING-IN-20 can be used for research on severe acute pancreatitis.
For research use only. We do not sell to patients.
- CAS No.: 1240287-64-2
- Formula: C27H30N6O3
- Molecular Weight:486.57
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Storage:
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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
STING 0.699 μM (Kd) |
TBK1 |
IRF3 |
NLRP3 |
IL-1β |
In Vitro
STING-IN-20 (1-5 μM) inhibits 2′3′-cGAMP-induced phosphorylation of STING, TBK1, and IRF3 in THP-1 cells[1].
STING-IN-20 (1-5 μM; 6 h) inhibits 2′3′-cGAMP-induced STING oligomerization in THP-1 cells[1].
STING-IN-20 restores the phagocytic capacity of primary pancreatic macrophages exposed to Caerulein (HY-A0190)-conditioned medium[1].
STING-IN-20 inhibits mitochondrial transfer from macrophages to β cells under pancreatitis-associated conditions in primary macrophage-MIN6 co-cultures[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP-1 cells
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Concentration:0.125, 0.25, 0.5, 1, and 2 μM
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Incubation Time:2 h
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Result:Dose-dependently reduced 2′3′-cGAMP-induced IFNβ mRNA.
Substantially attenuated HT-DNA- and 2′3′-cGAMP-induced IL6 and IFNβ expression, whereas the LPS-induced transcriptional response remained largely unaffected.
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Cell Line:THP-1 cells
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Concentration:1, 2.5, and 5 μM
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Incubation Time:6 h preincubation before 2′3′-cGAMP
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Result:Markedly reduced the abundance of oligomeric STING species following 2′3′-cGAMP stimulation.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (6-8 weeks old)[1]
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Dosage:5 mg/kg, 10 mg/kg, and 20 mg/kg
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Administration:oral gavage
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Result:Substantially alleviated pancreatic acinar cell injury and necrosis and prominent neutrophilic infiltration, with preservation of pancreatic architecture at 5, 10, and 20 mg/kg.
Attenuated pancreatitis-associated body weight loss.
Substantially reduced the Caerulein/LPS-elevated serum amylase and lipase concentrations.
Markedly diminished pancreatic p-STING immunoreactivity by immunohistochemistry and immunofluorescence.
Reduced pancreatic p62 accumulation while decreasing p-STING fluorescence.
Chemical Information
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CAS No. 1240287-64-2
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Molecular Weight 486.57
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Formula C27H30N6O3
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SMILES
O=C(C)C(C=C1)=CC=C1N(CC2)CCN2C(C3CCN(C(C4=CC(C5=CC=CC=N5)=NN4)=O)CC3)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
STING-IN-20 Related Classifications
HY-190942 Related Classifications
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