1. Immunology/Inflammation
  2. STING
  3. STING antagonist-3

STING antagonist-3 是一种强效的 STING 拮抗剂,对人野生型 STINGIC50 值为 2.3 nM。STING antagonist-3 可抑制人野生型 STING 以及功能获得性 STING 突变体 N154S 和 V155M。STING antagonist-3 可抑制受刺激的人全血中 IFN‑α2a 的产生。STING antagonist-3 可抑制活化的人皮肤微血管内皮细胞 (HMVEC-d) 中 IP-10 的产生。STING antagonist-3 可用于自身免疫性疾病、自身炎症性疾病、干扰素病以及纤维化疾病的研究。

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STING antagonist-3

STING antagonist-3 Chemical Structure

CAS No. : 3106554-00-8

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  • 生物活性

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生物活性

STING antagonist-3 is a potent STING antagonist with an IC50 of 2.3 nM against human wild-type STING. STING antagonist-3 inhibits human wild-type STING and the gain-of-function STING mutants N154S and V155M. STING antagonist-3 suppresses IFN‑α2a production in stimulated human whole blood. STING antagonist-3 inhibits IP-10 production in activated human dermal microvascular endothelial cells (HMVEC-d). STING antagonist-3 can be used for the research of autoimmune diseases, autoinflammatory diseases, interferonopathies, and fibrotic disorders[1].

体外研究
(In Vitro)

STING antagonist-3 (Example 21) 可在竞争性 HTRF 结合实验中抑制人源野生型 STINGR232,其 IC50 为 2.3 nM[1]
STING antagonist-3 (100 μM; temperature ramp from 15°C to 95°C over 160 cycles) 可在 DSF 实验中稳定人源野生型 STING 蛋白,抵抗其热变性,对应的 ΔTm 为 29 K[1]
STING antagonist-3 (10 μM; 60 min (pre-incubation); 22 h (post-stimulation)) 可抑制人全血中 cGAMP 刺激的 IFNα2α 产生,其 IC50 为 0.029 μM[1]
STING antagonist-3 (预孵育 1 小时;刺激 6 小时) 可抑制人 HMVEC 细胞中 dsDNA 诱导的 IP-10 产生,其 IC50 为 6.8 nM[1]

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

分子量

577.72

Formula

C35H39N5O3

CAS 号
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
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  • 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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STING antagonist-3
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HY-185379
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