Butein

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.

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

Packaged under inert gas

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 2 weeks at -20°C.

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.

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