2. Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease PI3K/Akt/mTOR Apoptosis
  3. SHP2 Phosphatase Akt Apoptosis
  4. SHP2-IN-8

SHP2-IN-8 是一种高效、具有选择性和细胞活性的变构 SHP2 抑制剂，IC50 为 23 nM，Ki 为 22 nM。SHP2-IN-8 可逆的、非竞争性的。SHP2-IN-8 能引起显著的热位移，ΔTm 为 7.01 ℃。SHP2-IN-8 可诱导 Hela 细胞凋亡 (apoptosis)，抑制 AKT 的磷酸化。

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SHP2-IN-8 Chemical Structure

SHP2-IN-8 Chemical Structure

CAS No. : 1801692-60-3

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SHP2-IN-8 相关抗体

Top Publications Citing Use of Products

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SHP2-IN-8 is a highly potent, selective, and cellularly active allosteric SHP2 inhibitor with IC50 value of 23 nM and Ki of 22 nM. SHP2-IN-8 is reversible and noncompetitive. SHP2-IN-8 causes a significant thermal shift with the ΔTm of 7.01 ℃. SHP2-IN-8 induces the apoptosis and inhibits the phosphorylation of AKT in Hela cells[1].

IC50 & Target

IC50: 23 nM (SHP2)[1]
Ki: 22 nM (SHP2)[1]
体外研究
(In Vitro)

SHP2-IN-8 (compound TK-453) (0-100 μM; 48 hours) has moderate inhibitory effects on the proliferation of KYSE-70, Hela and THP-1 cells[1].
SHP2-IN-8 (0-30 μM; 24 hours) induces the apoptosis of Hela cells in a concentration-dependent manner[1].
SHP2-IN-8 (0-30 μM; 0-2 hour）concentration- and time-dependently inhibits the phosphorylation of AKT in Hela and KYSE-70 cell lines[1].

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

SHP2-IN-8 相关抗体:

Cell Proliferation Assay

Cell Line: Hela, KYSE-70, THP-1[1]
Concentration: 0, 1, 3, 10, 30 and 100 μM
Incubation Time: 48 hours
Result: Showed moderate inhibitory effects on the proliferation of KYSE-70, Hela and THP-1 cells at the concentrations of 30 and 100 μM.

Apoptosis Analysis

Cell Line: Hela[1]
Concentration: 0, 10 and 30 μM
Incubation Time: 24 hours
Result: Induced the apoptosis of Hela cells in a concentration-dependent manner.

Western Blot Analysis

Cell Line: Hela and KYSE-70[1]
Concentration: 0, 0.3, 1, 3, 10 and 30 μM; or 10 μM
Incubation Time: 2 hours; or 0, 5, 10, 15, 30, 60, 120 min
Result: Concentration- and time-dependently inhibited the phosphorylation of AKT in Hela and KYSE-70 cell lines.
分子量

398.35

Formula

C17H21Cl2N5S
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

SHP2-IN-8 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-81801692-60-3SHP2PhosphataseAktApoptosisSrc homology phosphatase 2PTPN11PKBProtein kinase BDephosphorylaseAminopyrazinesReversibleNoncompetitiveHelaKYSE-70Inhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-144396
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