| Description | TEPP-46 (ML265) is a potent PKM2 activator (AC50 : 92 nM) showing little or no effect on PKM1, PKL and PKR,induces tetramerization and reduces tumor formation and size in a mouse xenograft model. . |
| In vivo | At 50 mg/kg, ML-265 has been shown to reduce tumor size, weight, and occurrence in mice bearing H1299 cell xenografts in a model of human non-small cell lung carcinoma[1] |
| Synonyms | ML265 |
| molecular weight | 372.46 |
| Molecular formula | C17H16N4O2S2 |
| CAS | 1221186-53-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 50 mg/mL (134.24 mM) |
| References | 1. Walsh M J , Brimacombe K R , Anastasiou D , et al. ML265: A potent PKM2 activator induces tetramerization and reduces tumor formation and size in a mouse xenograft model[M]// Probe Reports from the NIH Molecular Libraries Program. PubMed, 2009. 2. Palsson-Mcdermott E , Curtis A , Goel G , et al. Pyruvate Kinase M2 Regulates Hif-1α Activity and IL-1β Induction and Is a Critical Determinant of the Warburg Effect in LPS-Activated Macrophages[J]. Cell Metabolism, 2015, 21(1):65-80. |
| Citations | 1. Deng H, Qian X, Zhang Y, et al.Metformin Increases the Response of Cholangiocarcinoma Cells to Gemcitabine by Suppressing Pyruvate Kinase M2 to Activate Mitochondrial Apoptosis.Digestive Diseases and Sciences.2024: 1-15. |