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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C24H21N5O2S
- 分子量:443.52
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
体外実験
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.
-
Cell Line:wild-type bone marrow-derived macrophages (BMDMs)
-
Concentration:1 μM
-
Incubation Time:1 h (pretreatment); 30-120 min (stimulation with 500 nM diABZI-3)
-
Result:Inhibited diABZI-induced phosphorylation of TBK1 and IRF3.
Blocked STING oligomerization, as shown by reduced STING oligomer bands in native gel immunoblots.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
-
分子量 443.52
-
分子式 C24H21N5O2S
-
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
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)