STING antagonist-3
STING antagonist-3 is a potent STING antagonist with an IC50 of 2.3 nM against human wild-type STING. STING antagonist-3 inhibits human wild-type STING and the gain-of-function STING mutants N154S and V155M. STING antagonist-3 suppresses IFN‑α2a production in stimulated human whole blood. STING antagonist-3 inhibits IP-10 production in activated human dermal microvascular endothelial cells (HMVEC-d). STING antagonist-3 can be used for the research of autoimmune diseases, autoinflammatory diseases, interferonopathies, and fibrotic disorders.
For research use only. We do not sell to patients.
- CAS No.: 3106554-00-8
- Formula: C35H39N5O3
- Molecular Weight:577.72
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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
In Vitro
STING antagonist-3 (Example 21) inhibits human wild-type STINGR232 with an IC50 of 2.3 nM in the competitive HTRF binding assay[1].
STING antagonist-3 (100 μM; temperature ramp from 15°C to 95°C over 160 cycles) stabilizes human wild-type STING protein against thermal denaturation with a ΔTm of 29 K in the DSF assay[1].
STING antagonist-3 (10 μM; 60 min (pre-incubation); 22 h (post-stimulation)) inhibits cGAMP-stimulated IFNα2α production in human whole blood with an IC50 of 0.029 μM[1].
STING antagonist-3 (1 h (pre-incubation); 6 h (stimulation)) inhibits dsDNA-stimulated IP-10 production in human HMVEC cells with an IC50 of 6.8 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 3106554-00-8
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Molecular Weight 577.72
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Formula C35H39N5O3
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SMILES
CC(N=C([C@@H]1CC[C@H](CC1)C(O)=O)C=C2)=C2N3C(C)=C(C(C)C)C(C4=CC=CC5=NN(C[C@H](O)C6=CC=CC=C6)C=C54)=N3
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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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Endothelial Tube Formation Assay
Endothelial tube formation assay evaluates the ability of endothelial cells to attach, migrate, align, and organize into capillary-like networks when cultured on gelled basement membrane extract or Matrigel; the readout is the morphology and quantity of tube-like networks, which reflects an in vitro endothelial morphogenesis step related to angiogenesis. Basement membrane extract/Matrigel provides laminin-rich extracellular matrix cues that support endothelial differentiation into capillary-like structures, but it can contain biologically active growth factors, so growth-factor-reduced matrix is preferred when testing defined angiogenic stimulators or inhibitors.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
STING antagonist-3 Related Classifications
HY-185379 Related Classifications
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Keywords
- STING antagonist-3
- 3106554-00-8
- STING antagonist3
- STING antagonist 3
- STING
- human STING
- human dermal microvascular endothelial cells
- N154S STING mutant
- human whole blood
- V155M STING mutant
- systemic lupus erythematosus
- type 1 interferonopathies
- cutaneous lupus
- interferon alpha 2α
- interferon gamma-induced protein 10
- Inhibitor
- inhibitor
- inhibit