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17-b-Hydroxywortmannin (HWT)

Catalog # CD0278

Price: 1 mg - $75; 5 mg - $95; 10 mg - $150; 25 mg - $295

Availability:  In stock



17-b-Hydroxywortmannin (LY 301497)


Off white solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. Purity: 99% by HPLC. CAS# 58053-83-1. Solubility: DMSO (100 mg/mL). Molecular Formula: C23H26O8. Molecular Weight: 430.5.



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 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 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.



References: 1. Norman, B. H. et al J. Med. Chem. 1996, 39, 1106; 2. Dodge, J. D. et al Bioorg. Med. Chem. Lett. 1995, 5, 1713. 3. Zask, A., et al. J. Med. Chem. 2008, 51, 1319; 4. Zhu, T., et al. J. Med. Chem. 2006, 49, 1373; 5. Gelas, P., et al. Biochem. J. 1992, 287, 67.





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Caution Not fully tested. For research use only. Not for human use.

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