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1995•Chemical and Pharmaceutical BulletinOpen access

17.BETA.-Hydroxy-16.ALPHA.-(125I)iodowortmannin, a Sensitive Labeling Agent for PI 3-Kinases.

Shinobu Honzawa, Masahisa Nakada, Hiroshi Kurosu, Osamu Hazeki, Toshiaki Katada, Masakatsu Shibasaki

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Abstract

To detect phosphatidylinositol (PI) 3-kinases with high sensitivity, we designed and prepared a radiolabeled derivative of wortmannin (1), a potent inhibitor of PI 3-kinases. The synthesized derivative, 17β-hydroxy-16α-[125I]iodowortmannin (7), showed an IC50 that was 100-fold higher than that of wortmannin itself and which bound to catalytic subunits of PI 3-kinases.

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To detect phosphatidylinositol (PI) 3-kinases with high sensitivity, we designed and prepared a radiolabeled derivative of wortmannin (1), a potent inhibitor of PI 3-kinases. The synthesized derivative, 17β-hydroxy-16α-[125I]iodowortmannin (7), showed an IC50 that was 100-fold higher than that of wortmannin itself and which bound to catalytic subunits of PI 3-kinases.

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Available abstract

To detect phosphatidylinositol (PI) 3-kinases with high sensitivity, we designed and prepared a radiolabeled derivative of wortmannin (1), a potent inhibitor of PI 3-kinases. The synthesized derivative, 17β-hydroxy-16α-[125I]iodowortmannin (7), showed an IC50 that was 100-fold higher than that of wortmannin itself and which bound to catalytic subunits of PI 3-kinases.

Key concepts: Wortmannin, Pi, Chemistry, Kinase, Phosphatidylinositol, Derivative (finance), Alpha (finance), IC50

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