Wortmannin (KY 12420), isolated from filamentous fungus Penicillium funiculosum, is a potent, irreversible, noncompetitive and specific inhibitor of phosphatidylinositol 3 kinase (PI3K) with an IC50 value of 2 ~ 4 nM both in a time- and concentration-dependent manner. Wortmannin inhibits myosin light chain kinase (IC50 = 170 nM) but has no inhibition against PI4K (up to 32 μM), PKC (up to 22 μM), c-src (up to 5.5 μM) or phosphoinositide-specific phospholipase C (up to 0.27 mM)[1-3]. Wortmannin also potently inhibits polo-like kinase 1 (PLK1) (IC50 = 5.8 nM) [4]. Wortmannin enhances radiation or serum withdrawal-induced apoptosis through the inhibition of PI3-K/Akt signal transduction cascade and blocks the antiapoptotic effect of cytokines [5-6]. Wortmannin also blocks many of the short-term metabolic effects induced by insulin receptor activation in isolated rat adipocytes without affecting the insulin receptor tyrosine kinase activity [7]. Wortmannin is such a common used cell biology reagent that has been applied to suppress DNA repair, receptor-mediated endocytosis, adipogenesis, angiogenesis, autophagy, cell proliferation or induce in vivo Alzheimer-like hyperphosphorylation of tau protein.
Chemical Properties
Cas No.: 19545-26-7
M. Wt.: 428.44
Formula: C23H24O8
Purity: >99%
Synonym: KY 12420, Antibiotic SL-2052
Chemical Name:(1S,6bR,9aS,11R,11bR)11-(Acetyloxy)-1,6b,7,8,9a,10,11,11b-octahydro-1-(methoxymethyl)-9a,11b-dimethyl-3H-