Adenanthin

Ферментативный ингибитор

This diterpenoid (FW = 484.63 g/mol; CAS 111917-59-0) from the leaves of Rabdosia adenantha, induces differentiation of acute promyelocytic leukemia (APL) cells. Adenanthin targets the conserved cysteine thiols of peroxiredoxins I and II (or Prx I and Prx II), inhibiting their peroxidase activities and consequently increasing cellular hydrogen peroxide. The latter leads to the activation of Extracellular signal-Regulated Kinases (ERKs) and increased transcription of CCAAT/enhancer-binding protein β (or C/EBPs), further contributing to differentiation. Adenanthin induces APL-like cell differentiation, represses tumor growth in vivo and prolongs the survival of mouse APL models that are sensitive and resistant to retinoic acid.