PHPS1

SKU: orb1218179

Description

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.

Key Properties

• CAS Number: 314291-83-3
• MW: 465.44
• Purity: >98% (HPLC)
• Formula: C₂₁H₁₅N₅O₆S
• SMILES: [O-][N+](Cc(cc1)ccc1C(NN(C1=O)c2ccccc2)=C1N=Nc1ccc(CS(O)(=O)=O)cc1)=O
• Target: Phospholipase
• Solubility: DMSO:Soluble

Bioactivity

• In Vivo:
  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.
• In Vitro:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PHPS 1 | PHPS-1

Quick Database Links

Gene Symbol

Phospholipase