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.
|Storage||Desiccate at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 506.59. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.97 mL||9.87 mL||19.74 mL|
|5 mM||0.39 mL||1.97 mL||3.95 mL|
|10 mM||0.2 mL||0.99 mL||1.97 mL|
|50 mM||0.04 mL||0.2 mL||0.39 mL|
References are publications that support the products' biological activity.
Kim et al (2007) Glyceraldehyde 3-phosphate dehydrogenase is a cellular target of the insulin mimic demethylasterriquinone B1. J.Med.Chem. 50 3423 PMID: 17595071
Salituro et al (2001) Discovery of a small molecule insulin receptor activator. Recent Prog.Horm.Res. 56 107 PMID: 11237209
Weber et al (2000) A novel insulin mimetic without a proliferative effect on vascular smooth muscle cells. J.Vasc.Surg. 32 1118 PMID: 11107083
Webster et al (2003) Signaling effects of demethylasterriquinone B1, a selective insulin receptor modulator. Chembiochem 4 379 PMID: 12740809
Wilkie et al (2001) The non-peptidyl fungal metabolite L-783,281 activates TRK neurotrophin receptors. J.Neurochem. 78 1135 PMID: 11553687
If you know of a relevant reference for Demethylasterriquinone B1, please let us know.
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Literature in this Area
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Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.