PHPS1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PHPS1 是 Shp2 的抑制剂。 PHPS1 可有效抑制白血病相关的 Shp2 突变体 Shp2-E76K 对 Erk1/2 的激活，并阻断多种人类肿瘤细胞系的贴壁依赖性生长。

PHPS1 is an inhibitor of Shp2. PHPS1 efficiently inhibits activation of Erk1/2 by the leukemia-associated Shp2 mutant, Shp2-E76K, and blocks the anchorage-independent growth of a variety of human tumor cell lines.

Cell Viability Assay 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 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.

Animal Model:Ldlr-/- (005061) mice 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.

PHPS 1 | PHPS-1

Metabolic Enzyme/Protease

Phospholipase

PTP1B|Shp-1|SHP-2

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314291-83-3

465.44

C21H15N5O6S

>98% (HPLC)

DMSO:Soluble

[O-][N+](Cc(cc1)ccc1C(NN(C1=O)c2ccccc2)=C1N=Nc1ccc(CS(O)(=O)=O)cc1)=O

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(-20℃)

With Ice Pack

≥ 2 years