Hydroxywortmannin

A cell-permeable Wortmannin 17β -Hydroxy analog (HWT) that acts as an irreversible PI 3-K inhibitor with an 8.4-fold higher potency than that of Wortmannin (IC50 = 0.5 and 4.2 nM, respectively) and inhibits mTOR only at much higher concentrations (IC50 = 0.193 µ M). Both Wortmannin and HWT covalently modify a conserved lysine residue (Lys833 in porcine PI 3-Kγ ) in the PI 3-K ATP binding pocket via their electrophilic furan ring at C-20 position. HWT is shown to effectively arrest the growth of LNCaP cells (IC50 = 1.464 µ M) in vitro, however, its high in vivo toxicity renders it unsuitable for tumor killing studies in mice. Also reported to inhibit late phase PLD-mediated PA production upon fMLP stimulation of human neutrophils. See also our product PX-866-17OH (Cat # CD0323) and PX-13-17OH (Cat # CD0305) with similar activity.

58053-83-1

C₂₃H₂₆O₈

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