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  4. (2Z,3Z)-U0126

(2Z,3Z)-U0126 是 MEK1 和 MEK2 的选择性抑制剂，通过非竞争性抑制 AP-1 转录活性表现出强效抗炎作用，MEK1 的 IC50 值为 72 nM，MEK2 的 IC50 值为 58 nM。(2Z,3Z)-U0126 还通过阻断细胞外信号调节激酶和哺乳动物雷帕霉素靶蛋白途径来抑制 Ki-ras 转化大鼠成纤维细胞的锚定非依赖性生长。此外，(2Z,3Z)-U0126 可以进行异构化和环化，从而产生各种与母体化合物相比对 MEK 的亲和力降低且 AP-1 抑制作用减弱的产品。

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(2Z,3Z)-U0126 Chemical Structure

(2Z,3Z)-U0126 Chemical Structure

CAS No. : 218601-62-8

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(2Z,3Z)-U0126 相关抗体

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  • 生物活性

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生物活性

(2Z,3Z)-U0126 is a selective inhibitor of MEK1 and MEK2, demonstrating potent antiinflammatory effects by noncompetitively inhibiting AP-1 transcriptional activity with IC50 values of 72 nM for MEK1 and 58 nM for MEK2. (2Z,3Z)-U0126 also inhibits anchorage-independent growth of Ki-ras-transformed rat fibroblasts by blocking both the extracellular signal-regulated kinase and mammalian target of rapamycin pathways. Additionally, (2Z,3Z)-U0126 can undergo isomerization and cyclization, resulting in various products that show reduced affinity for MEK and diminished AP-1 inhibition compared to the parent compound.

分子量

380.49

Formula

C18H16N6S2
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

(2Z,3Z)-U0126 相关分类

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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.

Keywords:

(2Z,3Z)-U0126218601-62-8OthersInhibitorinhibitorinhibit

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产品名称：
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