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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- Formule: C24H21N5O2S
- Masse moléculaire:443.52
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Activité biologique
Description
In Vitro
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.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Masse moléculaire 443.52
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
UM-200 Related Classifications
HY-182923 Related Classifications
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