Chemical Name: 2-[2-(1,1-Dimethyl-2-propenyl)-1H-indol-3-yl]-3,6-dihydroxy-5-[7-(3-methyl-2-butenyl)-1H-indol-3-yl]-2,5-cyclohexadiene-1,4-dione
Biological ActivityDemethylasterriquinone B1 is a selective insulin receptor (IR) activator (EC50 values are 3 - 6 μM for IRTK and 100 μM for IGF1R and EGFR). Increases IR β subunit tyrosine phosphorylation and 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. Also activates Trk by interacting at a site distinct from the neurotrophin-binding site.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
The non-peptidyl fungal metabolite L-783,281 activates TRK neurotrophin receptors.
Wilkie et al.
Glyceraldehyde 3-phosphate dehydrogenase is a cellular target of the Ins mimic demethylasterriquinone B1.
Kim et al.
Discovery of a small molecule Ins receptor activator.
Salituro et al.
Recent Prog.Horm.Res., 2001;56:107
A novel Ins mimetic without a proliferative effect on vascular smooth muscle cells.
Weber et al.
Signaling effects of demethylasterriquinone B1, a selective Ins receptor modulator.
Webster et al.
Citation for Demethylasterriquinone B1
The citations listed below are publications that use Tocris products. Selected citations for Demethylasterriquinone B1 include:
1 Citation: Showing 1 - 1
Neuroprotective astrocyte-derived Ins/IGF-1 stimulates endocytic processing and extracellular release of neuron-bound Aβ oligomers.
Authors: Pitt Et al.
Mol Biol Cell 2017;28:2623
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