STING Degrader-2
STING Degrader-2 is an orally active STING degrader that promotes proteasome-independent degradation of STING. STING Degrader-2 inhibits cGAMP-induced STING activation, suppresses STING oligomerization, and inhibits phosphorylation of STING and interferon regulatory factor 3 (IRF3). STING Degrader-2 reduces serum IFN-β and CXCL-10 levels in a cGAMP-induced autoimmune disease mouse model. STING Degrader-2 can be used for the research of autoimmune diseases.
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- Formule: C43H39FN4O8S
- Masse moléculaire:790.86
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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
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Activité biologique
Description
In Vitro
STING Degrader-2 (compound SI-43) (6 h) inhibits cGAMP-induced STING activation in THP1-Blue ISG cells with an IC50 of 0.11 μM[1].
STING Degrader-2 (1 μM; 22 h after 2 h inhibitor pretreatment) induces degradation of STINGM155 in THP1 (STINGM155) cells via a proteasome-independent, lysosome-dependent pathway[1].
STING Degrader-2 (0.05-2.5 μM; 6 h) significantly reduces IFN-β and CXCL-10 secretion in THP1 cells and bone marrow-derived macrophages[1].
STING Degrader-2 (0.1-1 μM; 6-9 h) inhibits cGAMP-induced
phosphorylation of IRF3 and STING, as well as STING dimerization and oligomerization in THP1-Blue ISG cells[1].
STING Degrader-2 (0.01-10 μM; 6-48 h) induces degradation of mutants STINGS154 and STINGM155, while sparing STINGR232 and mSTING in THP1 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-Blue ISG cells
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Concentration:0.1; 1 μM
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Incubation Time:6; 9 h
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Result:Decreased cGAMP-induced
phosphorylation of IRF3 and STING.
Induced STING dimerization and oligomerization.
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Cell Line:THP1 cells; BMDM
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Concentration:0.05; 0.5; 2.5 μM
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Incubation Time:6 h
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Result:Significantly reduced IFN-β and CXCL-10 secretion in THP1 cells and BMDM isolated from mice, at 0.05 and 0.5 μM.
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Cell Line:THP1 cells harboring STINGS154, STINGM155, STINGR232, or mSTING
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Concentration:0.01; 0.1; 0.5; 1; 5; 10 μM
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Incubation Time:6; 12; 24; 48 h
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Result:Induced degradation of mutants STINGS154 and STINGM155, while sparing STINGR232 and mSTING in THP1 cells.
Demonstrated low inhibition activity against STINGM155 in THP1 cells.
Parmacokinetics
| Species | Dose | Route | Cmax | T1/2 | AUC | CL/F |
|---|---|---|---|---|---|---|
| Mice[1] | 20 mg/kg | p.o. | 293 ng/mL | 3.3 h | 2022.7 ng·h/mL | 9762.0 mL/h/kg |
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/6 mice with cGAMP-induced autoimmune disease[1]
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Dosage:20 mg/kg (p.o.); 10 mg/kg (s.c.)
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Administration:p.o. or s.c.; single dose
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Result:Significantly reduced cGAMP-induced serum IFN-β levels.
Significantly reduced cGAMP-induced serum CXCL-10 levels.
Chemical Information
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Masse moléculaire 790.86
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Formule C43H39FN4O8S
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SMILES
O=C(NC1=CC(NS(=O)(C)=O)=C(O)C=C1)C2=CC=C(C3=CC4=C(C=C3)OC(C(C(C(N)=O)C5=C6C=C(OC)C=C5)N(C7=CC(F)=C(C(C)(C)C)C=C7)C6=O)=C4)C=C2
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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 Degrader-2 Related Classifications
HY-174136 Related Classifications
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