Wortmannin 

Potent and specific phosphatidylinositol 3-kinase (PI3-K) inhibitor with an IC₅₀ of 2-4 nM. Inhibition of PI3-K/Akt signal transduction cascade enhances the apoptotic effects of radiation or serum withdrawal and blocks the antiapoptotic effect of cytokines. Inhibition of PI3-K by wortmannin also blocks many of the short-term metabolic effects induced by insulin receptor activation.

from Penicillium funiculosum

from Penicillium funiculosum

≥98% (HPLC and TLC)

powder

off-white

DMSO: soluble

H₂O: unstable

human ... PIK3CD(5293), PIK3CG(5294), PIK3R1(5295)

2-8°C

Powis, G., et al., Wortmannin, a potent and selective inhibitor of phosphatidylinositol-3-kinase. Cancer Res., (1994)

Wymann, M.P., et al., Wortmannin inactivates phosphoinositide 3-kinase by covalent modification of Lys-802, a residue involved in the phosphate transfer reaction. Mol. Cell. Biol. 16, 1722-1733, (1996) abstract

Nakanishi, S., Wortmann a microbial product inhibitor of myosin light chain kinase. J. Biol. Chem. 267, 2157, (1992) abstract

Krasilnikov, M., et al., Contribution of phosphatidylinositol 3-kinase to radiation resistance in human melanoma cells. Mol. Carcinog. 24, 64-69, (1999) abstract

Morita, Y., et al., Requirement for phosphatidylinositol-3'-kinase in cytokine-mediated germ cell survival during fetal oogenesis in the mouse. Endocrinology 140, 941-949, (1999) abstract

Crowder, R.J., and Freeman, R.S., Phosphatidylinositol 3-kinase and Akt protein kinase are necessary and sufficient for the survival of nerve growth factor-dependent sympathetic neurons. J. Neurosci. 18, 2933-2943, (1998) abstract

Moule, S.K., Denton, R.M., Multiple signaling pathways involved in the metabolic effects of insulin. Am. J. Cardiol. 80, 41, (1997)

Manna, S.K., Aggarwal, B.B., Interleukin-4 down-regulates both forms of tumor necrosis factor receptor and receptor-mediated apoptosis NFκB, AP-1and c-Jun N-terminal kinase. J. Biol. Chem. 273, 33333, (1998) abstract

Allen, M.P., et al., Growth arrest-specific gene 6/adhesion related kinase signaling promotes gonadotropin-releasing hormone neuronal survival via extracellular signal-regulated kinase (ERK) and Akt. Mol. Endocrinol. 13, 191-201, (1999) abstract

Merck 13,10110

Beil. 19,IV,3134

UN3462 6.1/PG 1

3

CB9641000