PKM2 inhibitor

  • Chemical Properties
CAS No. 94164-88-2 Cat. No. BCP23555
Name PKM2 inhibitor
Synonyms MDK4882; MDK-4882; MD K4882;PKM2-IN-1;
Formula C18H19NO2S2 M. Wt 345.48
  • Biological Activity
Description PKM2 inhibitor also known as MDK4882 or PKM2-IN-1 , is a PKM2 inhibitor. MDK4882 was first described in Eur J Med Chem. 2017;138:343-352. Currently there is no formal name. We temporally name it as MDK4882 for the convenience of communication, in which the last 4 digit of CAS# is used. MDK4882 displayed potent PKM2 inhibitory activity than the reported optimal PKM2 inhibitor shikonin. MDK4882 also showed nanomolar antiproliferative activity toward a series of cancer cell lines with high expression of PKM2 including HCT116, Hela and H1299 with IC50 values ranging from 0.18 to 1.56 μM. MDK4882 exhibited more cytotoxicity on cancer cells than normal cells.
Pathways Protease/Metabolic Enzyme 
Targets Pyruvate Kinase 

Structure

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