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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 | Availability | Quantity |
---|---|---|---|
1 mg | $84 | In Stock | |
5 mg | $198 | In Stock | |
10 mg | $347 | In Stock | |
25 mg | $668 | In Stock | |
50 mg | $987 | In Stock | |
100 mg | $1,330 | 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), PPARβ:~1 μM (EC50), PTP1B:1.6 μM, IKK-β: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] |
Alias | 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) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 80 mg/mL (142.98 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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