1. Metabolic Enzyme/Protease
  2. Phosphatase
  3. PHPS1 sodium

PHPS1 sodium 

Cat. No.: HY-125108
Handling Instructions

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.

For research use only. We do not sell to patients.

PHPS1 sodium Chemical Structure

PHPS1 sodium Chemical Structure

CAS No. : 1177131-02-0

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Description

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]

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.
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.
Molecular Weight

487.42

Formula

C₂₁H₁₄N₅NaO₆S

CAS No.

1177131-02-0

SMILES

O=S(C1=CC=C(C=C1)/N=N/C2C(C3=CC=C(C=C3)[N+]([O-])=O)=NN(C2=O)C4=CC=CC=C4)(O[Na])=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

PHPS1PHPS 1PHPS-1PhosphataseShp2Shp1PTP1BErk1/2atherosclerosiscancercoloncarcinomaprostatelungkidneyInhibitorinhibitorinhibit

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PHPS1 sodium
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