203987

Butein

A cell-permeable, reversible, substrate competitive, plant polyphenol that acts as a specific protein tyrosine kinase inhibitor.

• 別名: Butein, 2ʹ,4ʹ,3,4-Tetrahydroxychalcone
• 実験式（ヒル表記法）: C₁₅H₁₂O₅
• CAS番号: 487-52-5
• 分子量: 272.25
• MDL番号: MFCD00017300
• UNSPSCコード: 12352200

特性

• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• 形状: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: yellow
• 溶解性: DMSO: 10 mg/mL; methanol: soluble
• 輸送温度: ambient
• 保管温度: −20°C
• InChI: 1S/C15H12O5/c16-10-3-4-11(14(19)8-10)12(17)5-1-9-2-6-13(18)15(20)7-9/h1-8,16,18-20H/b5-1+
• InChI Key: AYMYWHCQALZEGT-ORCRQEGFSA-N

詳細

詳細

A cell-permeable, reversible, substrate competitive, plant polyphenol that acts as a specific protein tyrosine kinase inhibitor. Potently inhibits the tyrosine kinase activity of the EGF receptor (IC₅₀ = 65 µM) and p60^c-src (IC₅₀ = 65 µM) The inhibition is competitive with respect to ATP and non-competitive with respect to the substrate. Butein is also a potent antioxidant and anti-inflammatory agent. Has been shown to inhibit glutathione reductase (GSH-RD) and rat liver glutathione S-transferase (GST; IC₅₀ = 9 µM). Reported to activate sirtuins and promote the survival of eukaryotic cells.

A cell-permeable, reversible, substrate competitive, plant polyphenol that acts as a specific protein tyrosine kinase inhibitor. Potently inhibits the tyrosine kinase activity of the EGF receptor (IC₅₀ = 65 µM) and p60^c-src (IC₅₀ = 65 µM). The inhibition is competitive with respect to ATP and non-competitive with respect to the substrate. Butein is also a potent antioxidant and anti-inflammatory agent. Has been shown to inhibit glutathione reductase and rat liver glutathione-S-transferase (IC₅₀ = 9 µM). Reported to activate sirtuins and promote the survival of eukaryotic cells.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
Tyrosine kinase activity of the EGF receptor

Product competes with ATP.

Reversible: yes

Target IC₅₀: 65 µM against tyrosine kinase activity of the EGF receptor

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 2 weeks at -20°C.

その他情報

Howitz, K.T., et al. 2003. Nature425, 191.
Chan, S.C., et al. 1998. Planta Med.64, 153.
Yang, E.B., et al. 1998. Biochem. Biophys. Res. Commun. 245, 435.
Zhang, K., et al. 1997. Biochem. Pharmacol. 54, 1047.
Zhang, K., and Das, N.P. 1994. Biochem. Pharmacol. 47, 2063.

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