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.

• Synonyme(s) : PI 3-K Inhibitor XI, HWT, Wortmannin, 17β-Hydroxy, LY 301497, mTOR Inhibitor VIII
• Formule empirique (notation de Hill): C₂₃H₂₆O₈
• Numéro CAS: 58053-83-1
• Poids moléculaire : 430.45
• Code UNSPSC : 12352200

Propriétés

• Niveau de qualité: 100
• Pureté: ≥97% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: off-white
• Solubilité: DMSO: 100 mg/mL (Use only fresh DMSO.)
• Conditions d'expédition: ambient
• Température de stockage: 2-8°C

Description

Description générale

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.

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

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

Autres remarques

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.

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable