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Chemdea |
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17-b-Hydroxywortmannin
(HWT) |
Catalog # CD0278 |
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Price: 1 mg - $75; 5 mg - $95; 10 mg - $150; 25 mg - $295 |
Availability: In stock |
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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 µM). 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 µM) 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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CHEMDEA; |