2. Epigenetics Protein Tyrosine Kinase/RTK JAK/STAT Signaling Stem Cell/Wnt Apoptosis Autophagy
  3. JAK Apoptosis Autophagy
  4. Tubulosine

Tubulosine 是一种生物碱。Tubulosine 可从 Pogonopus tubulosus (DC.) Schumann 中分离得到。Tubulosine 是一种 ATP 竞争性的、选择性的 JAK3 抑制剂，其 IC50 值为 9.9 nM。Tubulosine 也能抑制其他 JAK 家族成员的激酶活性，但抑制程度低于 JAK3，对 JAK1、JAK2 和 TYK2 的 IC50 值分别为 69.5 nM、84.9 nM 和 76.3 nM。Tubulosine 通过与 JAK3 激酶的 ATP 结合位点结合，选择性地抑制 JAK3 信号通路。Tubulosine 可诱导凋亡 (Apoptotic) 和坏死/自噬性 (necrotic/autophagic) 细胞死亡。Tubulosine通过特异性地阻止延伸因子 2 依赖的易位步骤，抑制真核多聚核糖体肽链延伸过程。Tubulosine 在乳腺癌细胞中表现出抗癌活性。

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Tubulosine

Tubulosine Chemical Structure

CAS No. : 2632-29-3

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Tubulosine 相关抗体

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JAK1 JAK2 JAK3 Tyk2 JAK

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Tubulosine is an alkaloid. Tubulosine can be isolated from Pogonopus tubulosus (DC.) Schumann. Tubulosine is an ATP-competitive, selective JAK3 inhibitor with an IC50 value of 9.9 nM. Tubulosine also inhibits the kinase activities of other JAK family members, the extent of inhibition is less than that of JAK3, with IC50 values of 69.5, 84.9 and 76.3 nM for JAK1, JAK2 and TYK2, respectively. Tubulosine selectively inhibits JAK3 signalling by binding to the ATP-binding site of the kinase of JAK3. Tubulosine induces apoptotic and necrotic/autophagic cell death. Tubulosine inhibits the process of peptide chain elongation by eukaryotic polysomes by, specifically preventing the elongation-factor-2-dependent step of translocation. Tubulosine exhibits anticancer activity in breast cancer cells[1][2][3][4].

IC50 & Target[1][2][3][4]

JAK3

9.9 nM (IC50)

JAK1

69.5 nM (IC50)

JAK2

84.9 nM (IC50)

Tyk2

76.3 nM (IC50)

分子量

475.62

Formula

C29H37N3O3
CAS 号
结构分类
初始来源
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

Tubulosine 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

Tubulosine2632-29-3JAKApoptosisAutophagyJanus kinasebreast cancerInhibitorinhibitorinhibit

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