345834

Genistein, Soybean

A cell-permeable, reversible, substrate competitive inhibitor of protein tyrosine kinases, including autophosphorylation of epidermal growth factor receptor kinase (IC₅₀ = 2.6 µM).

• 同義詞: Genistein, Soybean, 4ʹ,5,7-Trihydroxyisoflavone
• 經驗公式（希爾表示法）: C₁₅H₁₀O₅
• CAS號碼: 446-72-0
• 分子量：: 270.24
• MDL號碼: MFCD00016952
• 分類程式碼代碼: 12352200
• NACRES: NA.77

屬性

• 品質等級: 100
• 化驗: ≥95% (HPLC)
• 形狀: solid
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: white
• 溶解度: DMSO: 200 mg/mL
• 運輸包裝: ambient
• 儲存溫度: −20°C
• InChI: 1S/C15H10O5/c16-9-3-1-8(2-4-9)11-7-20-13-6-10(17)5-12(18)14(13)15(11)19/h1-7,16-18H
• InChI 密鑰: TZBJGXHYKVUXJN-UHFFFAOYSA-N

描述

一般說明

A cell-permeable, reversible, substrate competitive inhibitor of protein tyrosine kinases, including autophosphorylation of epidermal growth factor receptor kinase (IC₅₀ = 2.6 µM). The inhibition is competitive with respect to ATP and non-competitive with respect to the phosphate acceptor. Has only a trivial effect on the activity of PKA and PKC (IC₅₀ >350 µM). Inhibits tumor cell proliferation and induces tumor cell differentiation. Produces cell cycle arrest and apoptosis in Jurkat T-leukemia cells. However, it prevents anti-CD3 monoclonal antibody-induced thymic apoptosis. Also inhibits topoisomerase II activity in vitro.

A cell-permeable, reversible, substrate competitive inhibitor of protein tyrosine kinases, including autophosphorylation of epidermal growth factor receptor kinase (IC₅₀ = 2.6 µM). The inhibition is competitive with respect to ATP and non-competitive with respect to the phosphate acceptor. Inhibits tumor cell proliferation and induces tumor cell differentiation. Inhibits exogenous substrate phosphorylation by EGFR kinase and pp60^v-src with similar potencies (IC₅₀ = 20-25 µM). Has only a trivial effect on PKC and PKA (IC₅₀ >350 µM). Produces cell cycle arrest and apoptosis in Jurkat T-leukemia cells. Prevents anti-CD3 monoclonal antibody-induced thymic apoptosis. Also inhibits topoisomerase II activity in vitro. Blocks oxidative DNA damage in vitro.

生化／生理作用

Cell permeable: yes

Primary Target
EGFR kinase

Product does not compete with ATP.

Reversible: yes

Target IC₅₀: 2.6 µM against autophosphorylation of epidermal growth factor receptor kinase

警告

Toxicity: Standard Handling (A)

其他說明

Constantinou, A., and Huberman, E. 1995. Proc. Soc. Exp. Biol. Med. 208, 109.
Wei, H., et al. 1995. Proc. Soc. Exp. Biol. Med. 208, 124.
Wei, H., et al. 1995. Carcinogenesis17, 73.
Kobayashi, S., et al. 1994. J. Biol. Chem.269, 9011.
Migita, K., et al. 1994. J. Immunol.153, 3457.
Spinozzi, F., et al. 1994. Leuk. Res.18, 431.
Dhar, A., et al. 1990. Mol. Pharmacol.37, 519.
Hill, T.D., et al. 1990. Science248, 1660.
Dean, N.M., et al. 1989. Biochem. Biophys. Res. Commun.165, 795.
Akiyama, T., et al. 1987. J. Biol. Chem.262, 5592.

法律資訊

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

安全資訊

• 象形圖: GHS07
• 訊號詞: Warning
• 危險聲明: H302
• 防範說明: P264 - P270 - P301 + P312 - P501
• 危險分類: Acute Tox. 4 Oral
• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable