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PI3K Inhibitor

No.172(January 2017)
W0007
Wortmannin   (1)
Autophagy is a catabolic process that digests components of the cytoplasm via lysosomes and is mediated by an organelle called the autophagosome.1,2) Autophagy is regulated by various serine/threonine protein kinases, such as mTOR, AKT, MARK etc.3) Phosphoinositide 3-kinases (PI3Ks) are also a class of such enzymes regulating autophagy. Especially, the class III PI3K promotes the formation of the autophagosome vesicle4) and a complex of the PI3K and beclin controls autophagy.5)
Wortmannin (1) is a potent PI3K inhibitor. Phosphatidylinositol 3,4,5-trisphosphate formation of fMLP-stimulated neutrophils is inhibited with a dose-responsive manner of 1 (IC50: 5 nM).6) It was shown that the treatment of rat hepatocytes with 1 inhibits autophagy with an IC50 of 30 nM.7)
It has been known that the properties of induced pluripotent stem cells (iPSCs), self-renewing and differentiation, make these cells tumorigenic.8) Zouboulis et al. reported that 1 can rapidly induce apoptosis in iPSCs.9) They discussed about apoptotic elimination of remaining undifferentiated iPSCs using 1 in their article.
mTOR: mammalian target of rapamycin
AKT: from the name of AKT8 retrovirus (J. Exp. Med. 1988, 167, 1259.)
MARK: mitogen-activated protein kinase
fMLP: N-formyl-L-methionyl-L-leucyl-L-phenylalanine
The product is for research purpose only.

References

Related Compounds

M2410
LY294002
I0975
PluriSIn 1
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