Demethylasterriquinone B1

Biological Activity

Demethylasterriquinone 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.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. The non-peptidyl fungal metabolite L-783,281 activates TRK neurotrophin receptors.
   Wilkie et al.
   J.Neurochem., 2001;78:1135
2. Glyceraldehyde 3-phosphate dehydrogenase is a cellular target of the Ins mimic demethylasterriquinone B1.
   Kim et al.
   J.Med.Chem., 2007;50:3423
3. Discovery of a small molecule Ins receptor activator.
   Salituro et al.
   Recent Prog.Horm.Res., 2001;56:107
4. A novel Ins mimetic without a proliferative effect on vascular smooth muscle cells.
   Weber et al.
   J.Vasc.Surg., 2000;32:1118
5. Signaling effects of demethylasterriquinone B1, a selective Ins receptor modulator.
   Webster et al.
   Chembiochem, 2003;4:379

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