Piperazine, 1-[(2,3-dihydro-1,4-benzodioxin-6-yl)sulfonyl]-4-[(4-methoxyphenyl)sulfonyl]-

Description

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.

Definition

ChEBI: 1-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-4-(4-methoxyphenyl)sulfonylpiperazine is a sulfonamide.

References

1) Boxer?et al., (2010),?Evaluation of N,N’-Diarylsulfonamides as Activators of the Tumor 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