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Ertiprotafib

Ertiprotafib
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.
Catalog No. T15243Cas No. 251303-04-5
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ee:100%
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Ertiprotafib

Catalog No. T15243Cas No. 251303-04-5

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.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
1 mg$84In Stock
5 mg$198In Stock
10 mg$347In Stock
25 mg$668In Stock
50 mg$987In Stock
100 mg$1,330In Stock
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Product Introduction

Bioactivity
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
PPARβ:~1 μM (EC50), IKK-β:400 nM, PPARα:~1 μM (EC50), PTP1B:1.6 μM
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]
AliasPTP 112, PTP112, PTP-112
Chemical Properties
Molecular Weight559.51
FormulaC31H27BrO3S
Cas No.251303-04-5
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM1.7873 mL8.9364 mL17.8728 mL89.3639 mL
5 mM0.3575 mL1.7873 mL3.5746 mL17.8728 mL
10 mM0.1787 mL0.8936 mL1.7873 mL8.9364 mL
20 mM0.0894 mL0.4468 mL0.8936 mL4.4682 mL
50 mM0.0357 mL0.1787 mL0.3575 mL1.7873 mL
100 mM0.0179 mL0.0894 mL0.1787 mL0.8936 mL

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