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Demethylasterriquinone B1
Chemical Name:2-[2-(1,1-Dimethyl-2-propenyl)-1H-indol-3-yl]-3,6-dihyd
roxy-5-[7-(3-methyl-2-butenyl)-1H-indol-3-yl]-2,5-cyclo
hexadiene-1,4-dione
Biological Activity:
Selective insulin receptor (IR)
activator/mimetic (EC50 values are 3-6 μM for IRTK
and 100 μM
for IGF-I-R and EGFR). Increases IR β subunit
tyrosine phosphorylation and downstream activation of PI 3-kinase and Akt, but
not ERK. Induces glucose uptake in adipocytes and skeletal muscle in vitro,
without enhancing vascular proliferation. Binds GAPDH.
Weberet al (2000)
A novel insulin mimetic without a proliferative effect on vascular smooth
muscle cells. J.Vasc.Surg. 32 1118. Salituroet al
(2001) Discovery of a small molecule insulin receptor activator. Recent
Prog.Horm.Res. 56 107. Websteret al (2003)
Signaling effects of demethylasterriquinone B1, a selective insulin receptor
modulator. Chembiochem 4 379. Kimet al (2007)
Glyceraldehyde 3-phosphate dehydrogenase is a cellular target of the insulin
mimic demethylasterriquinone B1. J.Med.Chem. 50 3423.
