1. Immunology/Inflammation
  2. STING
  3. UM-259 hydrochloride

UM-259 hydrochloride 是一种 STING 抑制剂,对小鼠和人源 STING (包括 STINGR232 突变体) 均具有活性。UM-259 hydrochloride 可抑制 STING 依赖性信号通路,阻断 STING 寡聚化,并作用于人原代 CD14+ 单核细胞。UM-259 hydrochloride 可用于肌萎缩侧索硬化症、红斑狼疮、Aicardi-Goutières 综合征及婴儿起病型 STING 相关性血管病的研究。

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UM-259 hydrochloride

UM-259 hydrochloride 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-259 hydrochloride is a STING inhibitor with activity against both murine and human STING (including the STINGR232 mutant). UM-259 hydrochloride inhibits STING-dependent signaling pathways, blocks STING oligomerization, and acts on human primary CD14+ monocytes. UM-259 hydrochloride can be used for research on amyotrophic lateral sclerosis, lupus erythematosus, Aicardi-Goutières syndrome, and infant-onset STING-associated vasculopathy[1].

体外研究
(In Vitro)

UM-259 hydrochloride (0.08-40 μM; 1 h +24 h;diABZI) 在 THP1-Dual KI-hSTING-R232 细胞中可抑制 STING 依赖性信号通路,其 EC50 为 1.50 μM[1]
UM-259 hydrochloride (0.2-5 μM; 1 h +2 h;diABZI) 可剂量依赖性地抑制 diABZI 诱导的 iBMDM 中 IFNβ 和 IL6 基因表达,在 5 μM 浓度下其效力优于 LB244 (HY-156117)[1]
UM-259 hydrochloride (0.2-5 μM; 1 h +24 h;diABZI) 可剂量依赖性地抑制 diABZI 诱导的 iBMDMs 中 IFNβ 的分泌,在 5 μM 时其效力优于 LB244[1]
UM-259 hydrochloride (2.5 μM; 1 h+16 h;diABZI) 可抑制 diABZI 诱导的原代人 CD14+ 单核细胞中 IFNβ 的分泌[1]
UM-259 hydrochloride (5 μM; 1 h+0-120 min; diABZI) 可抑制 diABZI 在野生型骨髓源性巨噬细胞 (BMDMs) 中诱导的 TBK1 和 IRF3 磷酸化[1]
UM-259 hydrochloride (5 μM; 1 h+30 min; diABZI) 可在野生型骨髓来源巨噬细胞 (BMDMs) 中阻断 diABZI 诱导的 STING 寡聚化[1]
UM-259 hydrochloride (0.2-5 μM; 24 h) 对 iBMDMs 仅表现出有限的细胞毒性[1]

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

ELISA Assay[1]

Cell Line: primary human CD14+ monocytes
Concentration: 2.5 μM
Incubation Time: 1 h pre-incubation, followed by 16 h incubation with diABZI
Result: Blocked diABZI-induced IFNβ secretion, reducing levels to near baseline (DMSO without diABZI) levels.

Western Blot Analysis[1]

Cell Line: wild-type bone marrow-derived macrophages (BMDMs)
Concentration: 5 μM
Incubation Time: 1 h pre-incubation, followed by 0-120 min incubation with diABZI
Result: Inhibited diABZI-induced phosphorylation of TBK1 and IRF3, reducing phosphorylated protein levels compared to vehicle-treated cells at all time points tested.
Blocked diABZI-induced STING oligomer formation, with only STING monomers detected in native fractions (similar to unstimulated cells), while vehicle-treated cells showed robust STING oligomer formation.
分子量

597.96

Formula

C27H22ClF2N7O5

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

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

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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-259 hydrochloride
目录号:
HY-178049A
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