| Name | Ertiprotafib |
| 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. |
| 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] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 80 mg/mL (142.98 mM), Sonication is recommended.
10% DMSO+90% Corn Oil : 3.3 mg/mL (5.9 mM), Sonication is recommended.
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| Keywords | PTP1B | PPARβ | PPARα | IκB | IKK-β | IKKβ | IKK | IkB/IKK | IkB | Ertiprotafib |
| Inhibitors Related | PHYTOL | Rosiglitazone | Daidzein | Hexane-1,6-diol | Magnesium acetate tetrahydrate | Maltitol | Cyclosporine | Stearic acid | L-Ascorbic acid 2-phosphate magnesium | 2,3-Butanediol | NPC 15199 | Cloxiquine |
| Related Compound Libraries | NF-κB Signaling Compound Library | Bioactive Compound Library | ReFRAME Related Library | Kinase Inhibitor Library | Anti-Ovarian Cancer Compound Library | Inhibitor Library | Metabolism Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Phosphatase Inhibitor Library | Anti-Cancer Active Compound Library | Transcription Factor-Targeted Compound Library |
United States
