| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 50mg | |||
| Other Sizes |
| Targets |
PHPS1 Sodium targets the protein tyrosine phosphatase Shp2 (Src homology 2 domain-containing phosphatase 2). Shp2 is a key signaling molecule that regulates various cellular processes, including cell proliferation, differentiation, and migration. PHPS1 Sodium is a potent and selective inhibitor of Shp2, with Kis of 0.73 µM for Shp2, 5.8 µM for Shp2-R362K, 10.7 µM for Shp1, 5.8 µM for PTP1B, and 0.47 µM for PTP1B-Q. By inhibiting Shp2, PHPS1 Sodium modulates downstream signaling pathways.
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| ln Vitro |
PHPS1 (30 μM; 6 days) prevents human tumor cells from proliferating [1]. In a dose-dependent manner, PHPS1 (5–20 μM; 5-360 min) suppresses Erk1/2 phosphorylation but not Akt or Stat3 [1].
In vitro, PHPS1 Sodium is a potent inhibitor of Shp2. It has been shown to inhibit the proliferation of various human tumor cells at a concentration of 30 µM over 6 days. PHPS1 specifically suppresses the phosphorylation of Erk1/2 in a dose-dependent manner, without affecting Akt and Stat3 phosphorylation. In a cell viability assay using various human cancer cell lines, a 30 µM concentration of PHPS1 resulted in varying reductions in cell numbers. These in vitro studies confirm PHPS1 Sodium's activity as a Shp2 inhibitor. |
| ln Vivo |
During the final week of a high-fat diet, PHPS1 (3 mg/kg; i.p.; daily) reduces the risk of atherosclerosis in Ldlr-/- mice [2].
In vivo, PHPS1 Sodium has been shown to reduce atherosclerosis susceptibility in LdIr -/- mice. At a dosage of 3 mg/kg administered intraperitoneally daily during the final week of a high-fat diet, a marked decrease in aortic atherosclerotic plaque size was observed compared to control groups. This suggests that PHPS1 Sodium may have potential therapeutic applications in cardiovascular disease. |
| Enzyme Assay |
In vitro enzyme assays for PHPS1 Sodium measure its inhibition of Shp2 phosphatase activity. Shp2 enzyme is incubated with a phosphopeptide substrate in the presence of varying concentrations of PHPS1 Sodium. The release of phosphate is measured, and the Ki is determined from the dose-response curve.
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| Cell Assay |
Cell viability assay [1]
Cell Types: human cancer cell lines MDA-MB-435, HCT-116 (colon cancer), HCT-15 (colon cancer), PC-3 (prostate cancer), HT-29 (colon cancer) , NCI-H661 (lung cancer) and Caki-1 (kidney cancer) Tested Concentrations: 30 μM Incubation Duration: 6 days Experimental Results: Caused a reduction in cell number from 0% (Caki-1) to 74% (HT-29). Western Blot Analysis[1] Cell Types: Madin-Darby canine kidney (MDCK) Cell Tested Concentrations: 5, 10, 20 μM Incubation Duration: 5, 15, 60, 120, 360 minutes Experimental Results: Inhibition of HGF/SF (1 unit/mL )) induces phosphorylation, thereby activating Erk1/2 over a period of 15 minutes to 6 hrs (hours). In contrast, transient phosphorylation of Erk1/2 was unaffected after 5 min. There was no effect on HGF/SF-induced activation of PI3K/Akt or Stat3. In vitro cell-based assays for PHPS1 Sodium are used to study its effects on Shp2-mediated signaling. Cells are treated with PHPS1 Sodium, and the phosphorylation of Erk1/2 and other downstream targets is measured by Western blotting. Cell proliferation is assessed using assays such as MTT or CellTiter-Glo. These assays confirm the compound's activity as a Shp2 inhibitor. |
| Animal Protocol |
Animal/Disease Models: Ldlr-/- (005061) mice[2]
Doses: 3 mg/kg Route of Administration: intraperitoneal (ip) injection; adhere to a high-fat diet every day for the past week. Experimental Results: The size of aortic atherosclerotic plaques was Dramatically diminished compared with the other two groups. In vivo animal experiments for PHPS1 Sodium have been conducted in mouse models of atherosclerosis. In a typical study, LdIr -/- mice are fed a high-fat diet and treated with PHPS1 Sodium (3 mg/kg, i.p.) daily during the last week of the diet. Atherosclerotic plaque size is measured in the aorta. These studies provide evidence for the in vivo efficacy of PHPS1 Sodium. |
| ADME/Pharmacokinetics |
PHPS1 Sodium has a molecular weight of 488.43 g/mol and a molecular formula of C21H15N5NaO6S. It has a CAS number of 1177131-02-0. It is a solid compound. For storage, it is recommended to keep the powder at -20°C for up to 3 years. In solvent, it can be stored at -80°C for 1 year. Detailed pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have not been extensively characterized.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for PHPS1 Sodium is not provided in standard product descriptions. As a research compound, its toxicity profile has not been extensively characterized. PHPS1 Sodium is a Shp2 inhibitor, and its toxicity would be related to its effects on Shp2-mediated signaling in normal tissues. As with all research chemicals, standard laboratory safety precautions should be followed.
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| References |
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| Additional Infomation |
PHPS1 Sodium is a research compound and is not approved for any clinical or therapeutic use. It is a potent and selective inhibitor of Shp2. It has Kis of 0.73 µM for Shp2, 5.8 µM for Shp2-R362K, 10.7 µM for Shp1, 5.8 µM for PTP1B, and 0.47 µM for PTP1B-Q. PHPS1 Sodium has been shown to inhibit the proliferation of various human tumor cells and to reduce atherosclerosis in a mouse model. It is a valuable research tool for studying the role of Shp2 in cell signaling and disease.
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| Molecular Formula |
C21H14N5NAO6S
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| Molecular Weight |
487.420533657074
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| CAS # |
1177131-02-0
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| Related CAS # |
PHPS1;314291-83-3
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| Appearance |
Brown to reddish brown solid powder
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| SMILES |
S(C1C=CC(=CC=1)/N=N/C1C(N(C2C=CC=CC=2)NC=1C1C=CC(=CC=1)[N+](=O)[O-])=O)(=O)(=O)[O-].[Na+]
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0516 mL | 10.2581 mL | 20.5162 mL | |
| 5 mM | 0.4103 mL | 2.0516 mL | 4.1032 mL | |
| 10 mM | 0.2052 mL | 1.0258 mL | 2.0516 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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