528119

PI 3-K Inhibitor XI, HWT

The PI 3-K Inhibitor XI, HWT, also referenced under CAS 58053-83-1, controls the biological activity of PI 3-K. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Sinónimos: PI 3-K Inhibitor XI, HWT, Wortmannin, 17β-Hydroxy, LY 301497, mTOR Inhibitor VIII
• Fórmula empírica (notación de Hill): C₂₃H₂₆O₈
• Número de CAS: 58053-83-1
• Peso molecular: 430.45
• UNSPSC Code: 12352200

Propiedades

• Quality Level: 100
• assay: ≥97% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: off-white
• solubility: DMSO: 100 mg/mL (Use only fresh DMSO.)
• shipped in: ambient
• storage temp.: 2-8°C

Descripción

General description

A cell-permeable Wortmannin (Cat. Nos. 681675 and 681676) 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 (Cat. No. 05-22-2500) stimulation of human neutrophils.

A cell-permeable Wortmannin (Cat. Nos. 681675 and 681676) 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 (Cat. No. 05-22-2500) stimulation of human neutrophils.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Zask, A., et al. 2008. J. Med. Chem.51, 1319.
Zhu, T., et al. 2006. J. Med. Chem.49, 1373.
Norman, B. H., et al. 1996. J. Med. Chem.39, 1106.
Gelas, P., et al. 1992. Biochem. J.287, 67.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Información de seguridad

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable