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Art. -Nr.: HY-174136

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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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₄₃H₃₉FN₄O₈S
Molecular Weight:790.86

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (273 KB)

STING Degrader-2 Chemical Structure

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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 STING^M155 in THP1 (STING^M155) 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 STING^S154 and STING^M155, while sparing STING^R232 and mSTING in THP1 cells^[1].

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

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 STING^S154, STING^M155, STING^R232, 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 STING^S154 and STING^M155, while sparing STING^R232 and mSTING in THP1 cells.
Demonstrated low inhibition activity against STING^M155 in THP1 cells.

Parmacokinetics

Species	Dose	Route	C_max	T_1/2	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.

Chemical Information

Molecular Weight 790.86
Formel 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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Zhao HY, et al. Design of Potent Small-Molecule Stimulator of Interferon Gene Inhibitor and Stimulator of Interferon Gene Mutant-Specific Degrader. J Med Chem. 2025;68(11):11100-11126. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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