2. Immunology/Inflammation
  3. STING IFNAR
  4. 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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STING Degrader-2

STING Degrader-2 Chemical Structure

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STING Degrader-2 Related Antibodies

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Description

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[1].

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.

STING Degrader-2 Related Antibodies

Western Blot Analysis[1]

Cell Line: THP1-Blue ISG cells
Concentration: 0.1; 1 μM
Incubation Time: 6; 9 h
Result: Decreased cGAMP-induced
phosphorylation of IRF3 and STING.
Induced STING dimerization and oligomerization.

ELISA Assay[1]

Cell Line: THP1 cells; BMDM
Concentration: 0.05; 0.5; 2.5 μM
Incubation Time: 6 h
Result: Significantly reduced IFN-β and CXCL-10 secretion in THP1 cells and BMDM isolated from mice, at 0.05 and 0.5 μM.

Western Blot Analysis[1]

Cell Line: THP1 cells harboring STINGS154, STINGM155, STINGR232, or mSTING
Concentration: 0.01; 0.1; 0.5; 1; 5; 10 μM
Incubation Time: 6; 12; 24; 48 h
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

STING Degrader-2 (compound SI-43) (10-20 mg/kg; p.o. or s.c.; single dose) demonstrates in vivo efficacy in cGAMP-induced autoimmune disease mouse model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice with cGAMP-induced autoimmune disease[1]
Dosage: 20 mg/kg (p.o.); 10 mg/kg (s.c.)
Administration: p.o. or s.c.; single dose
Result: Significantly reduced cGAMP-induced serum IFN-β levels.
Significantly reduced cGAMP-induced serum CXCL-10 levels.
Molecular Weight

790.86

Formula

C43H39FN4O8S
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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STING Degrader-2 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

STING Degrader-2STING Degrader2STING Degrader 2STINGIFNARStimulator of Interferon GenesTMEM173MITAERISMPYSInterferon-α/β receptorInterferon-alpha/beta receptorCXCL-10autoimmune disease mouse modelIRF3autoimmune diseasesIFN-βTHP1 (STING^M155) cellsSTING M155STING S154interferon regulatory factor 3Inhibitorinhibitorinhibit

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