Biological Activity:TEPP-46 (ML265) is a potent and selective Pyruvate kinase M2 (PKM2) activator with EC50 ~92 nM. It demonstrates >100-fold selectivity for PKM2 over the related PKM1, PKR, and PKL isoforms. It can stabilize pyruvate kinase subunit interactions, promote PKM2 tetramer formation and prevent inhibition by phosphotyrosine signaling. It can alter metabolism in cultured cells, and inhibit xenograft tumor growth in vivo. TEPP-46 inhibits LPS-induced Hif-1α and IL-1β, as well as the expression of a range of other Hif-1α-dependent genes.How to Use:In vitro: TEPP-46 was used at 1-10 µM final concentration in various assays. In vivo: TEPP-46 was dosed to mice orally at 50 mg/Kg twice per day. Reference:
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