Wortmannin

无

An irreversible PI3K inhibitor

By phosphorylating phosphatidylinositol, phosphoinositide 3-kinases (PI3K), activates diverse cellular functions, including cell growth, differentiation, survival, and motility. Wortmannin is a potent, cell-permeable, and irreversible inhibitor of PI3K enzymes (IC50 = 1-10 nM). However, the class II PI3Ks from Drosophila, murine, and human differ in sensitivity to wortmannin (IC50s = 5, 50, 450 nM, respectively).1 Wortmannin also inhibits polo-like kinase 1 (IC50 = 24 nM) and polo-like kinase 3 (IC50 = 49 nM), as well as mTOR, DNA-PK, PI4K, MLCK, and p38 MAPK at 50 to 100 fold higher concentrations than that needed for PI3K inhibition.2,3

428.4

≥98%

KY 12420

COC[C@H]1OC(=O)c2coc3C(=O)C4=C([C@H](OC(=O)C)C[C@]5(C)C(=O)CCC45)[C@]1(C)c23

C23H24O8

19545-26-7

≥ 4 years

DMF: 10 mg/ml DMSO: 10 mg/ml DMSO:PBS (pH 7.2)(1:8): 0.1 mg/ml Ethanol: 0.1 mg/ml

1.Fruman, D.A.,Meyers, R.E. and Cantley, L.C. Phosphoinositide kinases. Annual Reviews of Biochemistry 67, 481-507 (2008).
2.Liu, Y.,Shreder, K.R.,Gai, W., et al. Wortmannin, a widely used phosphoinositide 3-kinase inhibitor, also potently inhibits mammalian polo-like kinase. Chemistry & Biology 12, 99-107 (2005).
3.Liu, Y.,Jiang, N.,Wu, J., et al. Polo-like kinases inhibited by wortmannin. Labeling site and downstream effects. The Journal of Biological Chemisty 282(4), 2505-2511 (2007).

2811