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。
| 生物活性 | PHPS1 sodium is a potent and selectiveShp2inhibitor withKis of 0.73, 5.8, 10.7, 5.8, and 0.47 μM forShp2, 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].
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. |
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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].
| 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. |
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| 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) |
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