BML283 | PKM2 activator

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.

References/Citations
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