标签归档：phps

PHPS1 sodium

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PHPS1 sodium  纯度: ≥98.0%

PHPS1 sodium 是一种有效的选择性 Shp2 抑制剂，对 Shp2，Shp2-R362K，Shp1，PTP1B 和 PTP1B-Q 的 Ki 值分别为 0.73，5.8，10.7，5.8 和 0.47 μM。

PHPS1 sodium

PHPS1 sodium Chemical Structure

规格 价格 是否有货
5 mg ￥3800 询问价格 & 货期

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PHPS1 sodium 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Anti-Cardiovascular Disease Compound Library
  • Phosphatase Inhibitor Library
  • Anti-Obesity Compound Library

生物活性

PHPS1 sodium is a potent and selective Shp2 inhibitor with Kis of 0.73, 5.8, 10.7, 5.8, and 0.47 μM for Shp2, Shp2-R362K, Shp1, PTP1B, and PTP1B-Q, respectively[1].

IC50 & Target

Ki: 0.73 μM (Shp2), 5.8 μM (Shp2-R362K), 10.7 μM (Shp1), 5.8 μM (PTP1B), 0.47 μM (PTP1B-Q)[1]
体外研究
(In Vitro)

PHPS1 (30 μM; 6 days) inhibits proliferation of human tumor cells[1].
PHPS1 (5-20 μM; 5-360 minutes) inhibits Erk1/2 but not Akt and Stat3 phosphorylation in a dose-dependent manner[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Human cancer cell lines MDA-MB-435, HCT-116 (colon carcinoma), HCT-15 (colon carcinoma), PC-3 (prostate carcinoma), HT-29 (colon carcinoma), NCI-H661 (lung carcinoma), and Caki-1 (kidney carcinoma)
Concentration: 30 μM
Incubation Time: 6 days
Result: Resulted in a reduction in cell number of between 0% (Caki-1) to 74% (HT-29).

Western Blot Analysis[1]

Cell Line: Madin-Darby canine kidney (MDCK) cells
Concentration: 5, 10, 20 μM
Incubation Time: 5, 15, 60, 120, 360 minutes
Result: Inhibited HGF/SF (1 unit/mL)-induced phosphorylation and thus activation of Erk1/2 over a time period of 15 min to 6 h. In contrast, transient phosphorylation of Erk1/2 after 5 min was not affected.
Exhibited no effect on HGF/SF-induced activation of PI3K/Akt or Stat3.

体内研究
(In Vivo)

PHPS1 (3 mg/kg; i.p. injection; every day during the last week on the high-fat diet) renders Ldlr-/- mice less susceptible to atherosclerosis development[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Ldlr-/- (005061) mice[2]
Dosage: 3 mg/kg
Administration: Intraperitoneal (i.p.) injection; every day during the last week on the high-fat diet.
Result: Revealed a significant decrease in atherosclerotic plaque size in the aorta compared with the other two groups.

分子量

487.42

Formula

C21H14N5NaO6S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献

  • [1]. Klaus Hellmuth, et al. Specific Inhibitors of the Protein Tyrosine Phosphatase Shp2 Identified by High-Throughput Docking. Proc Natl Acad Sci U S A. 2008 May 20;105(20):7275-80.

    [2]. Jia Chen, et al. SHP2 Inhibitor PHPS1 Protects Against Atherosclerosis by Inhibiting Smooth Muscle Cell Proliferation. BMC Cardiovasc Disord. 2018 Apr 27;18(1):72.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

PHPS1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PHPS1 

PHPS1 是一种有效的选择性 Shp2 抑制剂，对 Shp2，Shp2-R362K，Shp1，PTP1B 和 PTP1B-Q 的 Ki 值分别为 0.73，5.8，10.7，5.8 和 0.47 μM。

PHPS1

PHPS1 Chemical Structure

CAS No. : 314291-83-3

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

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生物活性

PHPS1 is a potent and selective Shp2 inhibitor with Kis of 0.73, 5.8, 10.7, 5.8, and 0.47 μM for Shp2, Shp2-R362K, Shp1, PTP1B, and PTP1B-Q, respectively[1].

IC50 & Target

Ki: 0.73 μM (Shp2), 5.8 μM (Shp2-R362K), 10.7 μM (Shp1), 5.8 μM (PTP1B), 0.47 μM (PTP1B-Q)[1]
体外研究
(In Vitro)

PHPS1 (30 μM; 6 days) inhibits proliferation of human tumor cells[1].
PHPS1 (5-20 μM; 5-360 minutes) inhibits Erk1/2 but not Akt and Stat3 phosphorylation in a dose-dependent manner[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Human cancer cell lines MDA-MB-435, HCT-116 (colon carcinoma), HCT-15 (colon carcinoma), PC-3 (prostate carcinoma) HT-29 (colon carcinoma), NCI-H661 (lung carcinoma), and Caki-1 (kidney carcinoma)
Concentration: 30 μM
Incubation Time: 6 days
Result: Resulted in a reduction in cell number of between 0% (Caki-1) to 74% (HT-29).

Western Blot Analysis[1]

Cell Line: Madin-Darby canine kidney (MDCK) cells
Concentration: 5, 10, 20 μM
Incubation Time: 5, 15, 60, 120, 360 minutes
Result: Inhibited HGF/SF (1 unit/mL)-induced phosphorylation and thus activation of Erk1/2 over a time period of 15 min to 6 h. In contrast, transient phosphorylation of Erk1/2 after 5 min was not affected.
Exhibited no effect on HGF/SF-induced activation of PI3K/Akt or Stat3.

体内研究
(In Vivo)

PHPS1 (3 mg/kg; i.p. injection; every day during the last week on the high-fat diet) renders Ldlr-/- mice less susceptible to atherosclerosis development[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Ldlr-/- (005061) mice[2]
Dosage: 3 mg/kg
Administration: Intraperitoneal (i.p.) injection; every day during the last week on the high-fat diet.
Result: Revealed a significant decrease in atherosclerotic plaque size in the aorta compared with the other two groups.

分子量

465.44

Formula

C21H15N5O6S
CAS 号

314291-83-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献

  • [1]. Klaus Hellmuth, et al. Specific Inhibitors of the Protein Tyrosine Phosphatase Shp2 Identified by High-Throughput Docking. Proc Natl Acad Sci U S A. 2008 May 20;105(20):7275-80.

    [2]. Jia Chen, et al. SHP2 Inhibitor PHPS1 Protects Against Atherosclerosis by Inhibiting Smooth Muscle Cell Proliferation. BMC Cardiovasc Disord. 2018 Apr 27;18(1):72.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务