1. Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease
  2. SHP2 Phosphatase
  3. PHPS1

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.

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

PHPS1 Chemical Structure

PHPS1 Chemical Structure

CAS No. : 314291-83-3

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of PHPS1:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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]

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].

MedChemExpress (MCE) 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.
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].

MedChemExpress (MCE) 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.
Molecular Weight

465.44

Formula

C21H15N5O6S

CAS No.
Appearance

Solid

Color

Red to reddish brown

SMILES

O=S(C1=CC=C(N/N=C2C(C3=CC=C([N+]([O-])=O)C=C3)=NN(C4=CC=CC=C4)C\2=O)C=C1)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (53.71 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1485 mL 10.7425 mL 21.4850 mL
5 mM 0.4297 mL 2.1485 mL 4.2970 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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C1

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Volume (start)

V1

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C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1485 mL 10.7425 mL 21.4850 mL 53.7126 mL
5 mM 0.4297 mL 2.1485 mL 4.2970 mL 10.7425 mL
10 mM 0.2149 mL 1.0743 mL 2.1485 mL 5.3713 mL
15 mM 0.1432 mL 0.7162 mL 1.4323 mL 3.5808 mL
20 mM 0.1074 mL 0.5371 mL 1.0743 mL 2.6856 mL
25 mM 0.0859 mL 0.4297 mL 0.8594 mL 2.1485 mL
30 mM 0.0716 mL 0.3581 mL 0.7162 mL 1.7904 mL
40 mM 0.0537 mL 0.2686 mL 0.5371 mL 1.3428 mL
50 mM 0.0430 mL 0.2149 mL 0.4297 mL 1.0743 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
PHPS1
Cat. No.:
HY-112368
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