BML283 (562867-96-3) is a selective activator of the Tumor Specific M2 Isoform of Pyruvate Kinase (PKM2) - AC50 = 111nM.1 PKM2 activity is downregulated in most cancer cells leading to a decrease in catabolic metabolism and an increase in anabolic metabolism.2,3 BML283 is an important tool for studying the effects of PKM2 and cancer metabolism.
1) Boxer et al., (2010), Evaluation of N,N'-Diarylsulfonamides as Activators of theTumor Specific M2 Isoform of Pyruvate Kinase; J. Med. Chem., 53 1048
2) Israelsen et al. (2013), PKM2 Isoform-Specific Deletion Reveals A Differential Requirement for Pyruvate Kinase in Tumor Cells; Cell 155 397
3) Wong et al. (2015), PKM2 contributes to cancer metabolism; Cancer Lett. 356 184