1. Immunology/Inflammation
  2. STING
  3. UM-200

UM-200 是一种共价的 STING 抑制剂,EC50 为 1.10 μM。UM-200 可共价修饰 STING 的半胱氨酸残基 C292 或 C309,从而阻断其寡聚化及下游信号传导。UM-200 可抑制 STING 依赖性的 TBK1IRF3 磷酸化。UM-200 可在小鼠体系中抑制 STING 信号通路。UM-200 可用于 STING 驱动的炎症及自身免疫性疾病的研究。

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UM-200

UM-200 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1].

体外研究
(In Vitro)

UM-200 (预处理 1 小时,刺激 24 小时,0.08-40 μM) 可强效抑制 THP1-Dual KI-hSTING-R232 细胞中的 STING 信号通路,其 EC50 为 1.10 μM[1]
UM-200 (预处理 1 小时,刺激 2 小时) 可抑制 diABZI 诱导的永生化骨髓来源巨噬细胞中 IFNβ 和 IL6 的基因转录[1]
UM-200 (预处理 1 小时,刺激 24 小时) 可抑制永生化骨髓来源巨噬细胞中 diABZI 诱导的 IFNβ 分泌[1]
UM-200 (2.5 μM; 1 h pretreatment, 16 h stimulation) 在剂量为 2.5 μM 时可抑制 diABZI 诱导的原代人 CD14+单核细胞中 IFNβ 的分泌[1]
UM-200 (1 μM; 1 h pretreatment, 30-120 min stimulation) 可抑制 diABZI 诱导的 TBK1 和 IRF3 磷酸化,并在以 1 μM 剂量作用时阻断野生型骨髓来源巨噬细胞中 STING 的寡聚化[1]
UM-200 在小鼠肝微粒体中比 LB244 更稳定[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

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.
体内研究
(In Vivo)

UM-200 能有效抑制小鼠系统中的 STING 信号传导[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

443.52

Formula

C24H21N5O2S

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
UM-200
目录号:
HY-182923
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