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Ertiprotafib (PTP 112), a selective and potent inhibitor of protein tyrosine phosphate 1B (PTP1B) and IkappaB kinase β (IKK-β), is a novel insulin sensitizer with potential anticancer activity for the study of type 2 diabetes and breast cancer.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $84 | In Stock | In Stock | |
| 5 mg | $198 | In Stock | In Stock | |
| 10 mg | $347 | In Stock | In Stock | |
| 25 mg | $668 | In Stock | In Stock | |
| 50 mg | $987 | In Stock | In Stock | |
| 100 mg | $1,330 | In Stock | In Stock |
| Description | Ertiprotafib (PTP 112), a selective and potent inhibitor of protein tyrosine phosphate 1B (PTP1B) and IkappaB kinase β (IKK-β), is a novel insulin sensitizer with potential anticancer activity for the study of type 2 diabetes and breast cancer. |
| Targets&IC50 | PPARα:~1 μM (EC50), PTP1B:1.6 μM, PPARβ:~1 μM (EC50), IKKβ:400 nM |
| In vitro | METHODS: To measure the kinase activity of IKK-b, ertiprotafib was used in doses (0.001-1 μM) and a peptide substrate containing the IjB phosphorylation motif was used, and the phosphorylated peptide product was determined using an ELISA-type assay with time-resolved fluorescence (TRF) measurements. RESULTS: Ertiprotafib is a potent IKK-b inhibitor with an IC50 value of 400 ± 40 nM, which is well below the value required for half-maximal inhibition of PTP1B p-nitrophenyl phosphatase activity. The reported IC50 values of ertiprotafib for PTP1B range from 1.6 to 29 μM, depending on the assay conditions. [1] |
| In vivo | METHODS: Here, 11-week-old leptin-deficient male ob/ob mice were administered Ertiprotafib (25 mg/kg, daily, for 4 days), and changes in blood glucose indicators were observed. RESULTS: Mice treated with ertiprotafib had fasting blood glucose levels returned to the normal range, along with a significant decrease in insulin levels and a significant decrease in serum triglyceride levels. [2] |
| Synonyms | PTP-112, PTP112, PTP 112 |
| Molecular Weight | 559.51 |
| Formula | C31H27BrO3S |
| Cas No. | 251303-04-5 |
| Smiles | CC=1C2=C(C=3C(C(Br)=C2SC1C)=CC=CC3)C4=CC(C)=C(O[C@H](CC5=CC=CC=C5)C(O)=O)C(C)=C4 |
| Relative Density. | 1.376 g/cm3 (Predicted) |
| Color | Yellow |
| Appearance | Solid |
| Storage | keep away from moisture,store under nitrogen,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 80 mg/mL (142.98 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+90% Corn Oil: 3.3 mg/mL (5.9 mM), Sonication is recommeded. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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