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M77976 is a specific ATP-competitive inhibitor of PDK4 (pyruvate dehydrogenase kinase isoforms 4), with an IC50 of 648 μM. M77976 binds to the ATP-binding pocket of PDK4 and causes local conformational changes with complete disordering of the ATP lid. M77976 makes hydrophobic interactions with the side chains of Asn258, Ala262, Val298, Leu306 and Thr358 of PDK4. M77976 is potential for the research of obesity and diabetes.
| Molecular Weight | 296.32 |
| Formula | C17H16N2O3 |
| CAS Number | 394237-61-7 |
| Solubility (25°C) | DMSO > 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PDHK Products |
|---|
| VER-246608
VER-246608 is a potent and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50s of 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK-4, respectively. |
| KPLH1130
KPLH1130 is a pyruvate dehydrogenase kinase (PDK)-specific inhibitor that blocks macrophage polarization, attenuates inflammatory responses, and improves glucose tolerance in mice fed a high-fat diet. |
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