PROTAC STING Degrader-2
PROTAC STING Degrader-2 is a STING PROTAC degrader with a DC50 of 0.53 μM. PROTAC STING Degrader-2 reduces the phosphorylation levels of TBK1 and IRF3. PROTAC STING Degrader-2 decreases the mRNA expression levels of IFN-β, CXCL10 and TNF-α, and blocks luciferase secretion. PROTAC STING Degrader-2 can be used in the research of autoimmune diseases.
For research use only. We do not sell to patients.
- CAS No.: 3023095-61-3
- Formula: C74H79FN10O15S3
- Molecular Weight:1463.67
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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
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Biological Activity
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VHL |
PROTAC STING Degrader-2 (Compound SD-02) (78 nM-20 μM; 24 h) dose-dependently degrades STING protein in THP1 cells, with a DC50 of 0.53 μM and a Dmax of 56.65%[1].
PROTAC STING Degrader-2 (0.25-2 μM; 24 h) dose-dependently inhibits SATE-3',3'-c-di-dAMP-induced phosphorylation of TBK1 and IRF3 in THP1 cells[1].
PROTAC STING Degrader-2 (0.25-2 μM; 24 h) dose-dependently inhibits the mRNA expression of IFN-β, CXCL10 and TNF-α in THP1 cells induced by SATE-3',3'-c-di-dAMP[1].
PROTAC STING Degrader-2 (24 h) inhibits SATE-3',3'-c-di-dAMP-induced STING pathway activation in THP-1 Lucia ISG cells, with an IC50 of 604 nM[1].
PROTAC STING Degrader-2 (24 h) exhibits no cytotoxicity against THP1, U937 or U2OS cells at concentrations that effectively degrade STING, and does not inhibit cell proliferation even at higher concentrations[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP1 cells
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Concentration:78 nM, 312 nM, 1.25 μM, 5 μM, 20 μM
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Incubation Time:24 h
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Result:Caused a dose-dependent decrease in STING protein levels, with a DC50 of 0.53 μM and a maximum degradation (Dmax) of 56.65%.
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Cell Line:THP1 cells
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Concentration:0.25 μM, 0.5 μM, 1 μM, 2 μM
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Incubation Time:24 h pre-incubation; 4 h SATE-3',3'-c-di-dAMP stimulation
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Result:Caused a dose-dependent reduction in SATE-3',3'-c-di-dAMP-induced phosphorylation of TBK1 and IRF3.
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Cell Line:THP1 cells
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Concentration:0.25 μM, 0.5 μM, 1 μM, 2 μM
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Incubation Time:24 h pre-incubation; 4 h SATE-3',3'-c-di-dAMP stimulation
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Result:Caused a dose-dependent decline in SATE-3',3'-c-di-dAMP-induced upregulation of IFN-β, CXCL10, and TNF-α mRNA levels.
Chemical Information
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CAS No. 3023095-61-3
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Molecular Weight 1463.67
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Formula C74H79FN10O15S3
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SMILES
CC1=C(SC=N1)C2=CC=C(C=C2)[C@@H](NC([C@@H]3C[C@H](CN3C([C@H](C(C)(C)C)NC(CCC(NCCCNC(C4=CC=CC(S(=O)(N5C=C(C=CC5=O)C(NCCCCCC(OC6=C(C=C(C=C6)NC(C7=CC=C(C=C7)C8=CC=CC=C8)=O)NS(=O)(C9=CC=C(C=C9)F)=O)=O)=O)=O)=C4)=O)=O)=O)=O)O)=O)C
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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)
PROTAC STING Degrader-2 Related Classifications
HY-158036 Related Classifications
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