2. Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR MAPK/ERK Pathway Stem Cell/Wnt Apoptosis
  3. SHP2 Akt ERK Apoptosis
  4. SHP2-IN-47

SHP2-IN-47 是一种选择性强效的 SHP2 抑制剂，其 IC50 为 0.80 μM。SHP2-IN-47 对 SHP2E76K 表现出强抑制活性，IC50 = 0.37 μM。SHP2-IN-47 可在功能上抑制蛋白酪氨酸磷酸酶结构域，并下调 SHP2 介导的 AKT 和 ERK 磷酸化水平。SHP2-IN-47 可诱导细胞凋亡 (apoptosis) 并抑制癌细胞增殖。SHP2-IN-47 可用于癌症研究，例如急性髓系白血病。

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SHP2-IN-47

SHP2-IN-47 Chemical Structure

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SHP2-IN-47 相关抗体

Top Publications Citing Use of Products

查看 Akt 亚型特异性产品:

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Akt Akt1 Akt2 Akt3

查看 ERK 亚型特异性产品:

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ERK ERK1 ERK2 ERK5 ERK8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SHP2-IN-47 is a selective and potent SHP2 inhibitor with an IC50 of 0.80 μM. SHP2-IN-47 exhibits potent inhibitory activity against SHP2E76K (IC50 = 0.37 μM). SHP2-IN-47 functionally inhibits protein tyrosine phosphatase domains and downregulates SHP2-mediated phosphorylation of AKT and ERK. SHP2-IN-47 induces apoptosis and suppresses proliferation of cancer cells. SHP2-IN-47 can be used for the research of cancer, such as acute myelocytic leukemia[1].

体外研究
(In Vitro)

SHP2-IN-47 (Compound A4) (30 min) 可强效抑制重组 SHP2WT (IC50 = 0.80 μM)、SHP2E76K (IC50 = 0.37 μM) 以及 SHP2-PTP 催化结构域 (IC50 = 0.32 μM)，但对 SHP1 或 PTP1B 无显著抑制作用[1]。
SHP2-IN-47 (3 days) 可抑制 MV-4-11 (IC50 = 2.12 μM)、KYSE520 (IC50 = 19.82 μM)、HCT116 (IC50 = 3.17 μM)、MDA-MB-231 (IC50 = 7.71 μM) 和 HepG2 (IC50 = 4.16 μM) 癌细胞系的增殖，且对 THP-1 来源的巨噬细胞毒性较低 (CC50 > 50 μM)[1]。
SHP2-IN-47 (2-6 μM; 24 h) 可在 MV-4-11 细胞中剂量依赖性地下调由 SHP2 介导的 AKT 和 ERK 的磷酸化水平[1]。
SHP2-IN-47 (2-6 μM; 24 h) 可剂量依赖性地诱导 MV-4-11 细胞发生凋亡[1]。

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

SHP2-IN-47 相关抗体:

Western Blot Analysis[1]

Cell Line: MV-4-11 cells
Concentration: 2, 4, 6 μM
Incubation Time: 24 h
Result: Reduced the phosphorylation levels of AKT (p-AKT) and ERK (p-ERK) in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: MV-4-11 cells
Concentration: 2, 4, 6 μM
Incubation Time: 24 h
Result: Induced apoptosis in a dose-dependent manner, with marked accumulation of cells in the late apoptotic (Annexin V+/PI+) stage.
分子量

738.75

Formula

C34H37Cl2N9O2S2
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

SHP2-IN-47 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

Keywords:

SHP2-IN-47SHP2AktERKApoptosisSrc homology phosphatase 2PTPN11PKBProtein kinase BExtracellular signal regulated kinasescolon canceracute myelocytic leukemiaprotein tyrosine phosphatase domainsAKTapoptosisSHP2WTtriple negative breast cancerSHP2E76Kesophageal squamous cell carcinomaInhibitorinhibitorinhibit

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