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Ertiprotafib

🥰Excellent
Catalog No. T15243Cas No. 251303-04-5
Alias PTP-112, PTP112, PTP 112

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.

Ertiprotafib

Ertiprotafib

🥰Excellent
Purity: 98.38%
Catalog No. T15243Alias PTP-112, PTP112, PTP 112Cas 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.
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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Purity:98.38%
ee:100%
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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
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]
AliasPTP-112, PTP112, PTP 112
Chemical Properties
Molecular Weight559.51
FormulaC31H27BrO3S
Cas No.251303-04-5
SmilesCC=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 & 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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