UM-200
UM-200 is a covalent STING inhibitor with an EC50 of 1.10 μM. UM-200 covalently modifies the cysteine residues C292 or C309 of STING, thereby blocking its oligomerization and downstream signal transduction. UM-200 inhibits STING-dependent phosphorylation of TBK1 and IRF3. UM-200 inhibits the STING signaling pathway in mouse models. UM-200 can be used for research on STING-driven inflammatory and autoimmune diseases.
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- Fòrmula: C24H21N5O2S
- Peso molecular:443.52
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Help & FAQs
Actividad biológica
UM-200 (0.08-40 μM; 1 h pretreatment, 24 h stimulation) potently inhibits STING signaling in THP1-Dual KI-hSTING-R232 cells with an EC50 of 1.10 μM[1].
UM-200 (1 h pretreatment, 2 h stimulation) inhibits diABZI-induced IFNβ and IL6 gene transcription in immortalized bone marrow-derived macrophages[1].
UM-200 (1 h pretreatment, 24 h stimulation) inhibits diABZI-induced IFNβ secretion in immortalized bone marrow-derived macrophages[1].
UM-200 (2.5 μM; 1 h pretreatment, 16 h stimulation) inhibits diABZI-induced IFNβ secretion in primary human CD14+ monocytes when dosed at 2.5 μM[1].
UM-200 (1 μM; 1 h pretreatment, 30-120 min stimulation) inhibits diABZI-induced phosphorylation of TBK1 and IRF3, and blocks STING oligomerization in wild-type bone marrow-derived macrophages when dosed at 1 μM[1].
UM-200 (1 μM; up to 45 min) exhibits improved metabolic stability in human liver microsomes with a half-life of 77 min[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:wild-type bone marrow-derived macrophages (BMDMs)
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Concentration:1 μM
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Incubation Time:1 h (pretreatment); 30-120 min (stimulation with 500 nM diABZI-3)
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Result:Inhibited diABZI-induced phosphorylation of TBK1 and IRF3.
Blocked STING oligomerization, as shown by reduced STING oligomer bands in native gel immunoblots.
Chemical Information
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Peso molecular 443.52
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Fòrmula C24H21N5O2S
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SMILES
O=C(C1=CN=C(S1)C2=CC=CC=C2)N[C@H](C3=NC4=C(N3C)C=CC=C4)CCNC(C#C)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
UM-200 Related Classifications
HY-182923 Related Classifications
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