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.

• 別名: PI 3-K Inhibitor XI, HWT, Wortmannin, 17β-Hydroxy, LY 301497, mTOR Inhibitor VIII
• 実験式（ヒル表記法）: C₂₃H₂₆O₈
• CAS番号: 58053-83-1
• 分子量: 430.45
• UNSPSCコード: 12352200

特性

• 品質水準: 100
• アッセイ: ≥97% (HPLC)
• フォーム: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: off-white
• 溶解性: DMSO: 100 mg/mL (Use only fresh DMSO.)
• 輸送温度: ambient
• 保管温度: 2-8°C

詳細

詳細

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.

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

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

その他情報

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.

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable