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PTP1B-IN-2 is a potent and selective protein tyrosine phosphatase-1B (PTP1B) inhibitor with IC50 of 50 nM. PTP1B-IN-2 displays more than 40-fold selectivity for PTP1B over SHP-2 and LAR and 15-fold higher selectivity for PTP1B over the highly homologous TCPTP. PTP1B-IN-2 extends deep into the active site pocket, forming several hydrogen bonds and hydrophobic interactions with key residues of the catalytic site. PTP1B-IN-2 greatly enhances insulin-mediated IRβ phosphorylation at concentrations of 15 µM and 30 µM. Insulin-stimulated glucose uptake is also significantly increased in L6 myotubes treated with PTP1B-IN-2, and this increase is 16.0%, 19.0% and 38.1% at 5, 10 and 20 µM, respectively.
| Molecular Weight | 680.79 |
| Formula | C34H36N2O9S2 |
| CAS Number | 1919853-46-5 |
| Solubility (25°C) | DMSO 70 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Phosphatase Products |
|---|
| CCT007093
CCT007093 is a potent PPM1D (WIP1) inhibitor with IC50 of 8.4 μM. |
| Microcystin-LR
Microcystin-LR is a potent protein phosphatase inhibitor with IC50 of 0.04 nM for PP2A, >40-fold selectivity over PP1. |
| Sal003
Sal003 is a potent and cell-permeable eIF-2α phosphatase inhibitor. |
| β-Glycerophosphate disodium salt hydrate
β-Glycerophosphate is a classical serine-threonine phosphatase inhibitor used in kinase reaction buffers. |
| Rhein-8-O-β-D-glucopyranoside
Rhein-8-glucoside calcium, a anthraquinone compound isolated from EtOH extract of Saussurea lappa root. Rhein-8-glucoside calcium is an hPTP1B inhibitor with an IC50 value of 11.5 μM. Rhein-8-glucoside calcium has antibacterial effects. |
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