Demethylasterriquinone B1 (Synonyms: DMAQ B1,L-783,281)

Demethylasterriquinone B1 (DMAQ B1) is a natural insulin mimic that activates insulin receptor tyrosine kinase (IRTK; EC50 = 6 µM).[1],[2],[3],[4] It less potently activates IGF1R and EGFR (EC50s = 100 µM for both). DMAQ B1 induces glucose uptake in adipocytes and skeletal muscle cells without activating proliferation. DMAQ B1 binds GAPDH in vitro.[5]

Reference:
[1]. Salituro, G.M., Pelaez, F., and Zhang, B.B. Discovery of a small molecule insulin receptor activator. Recent Prog. Horm. Res. 56, 107-126 (2001).
[2]. Tsai, H.J., and Chou, S.Y. A novel hydroxyfuroic acid compound as an insulin receptor activator. Structure and activity relationship of a prenylindole moiety to insulin receptor activation. J. Biomed. Sci. 16(68), (2009).
[3]. Weber, M.A., Lidor, A., Arora, S., et al. A novel insulin mimetic without a proliferative effect on vascular smooth muscle cells. J. Vasc. Surg. 32(6), 1118-1126 (2000).
[4]. Webster, N.J.G., Park, K., and Pirrung, M.C. Signaling effects of demethylasterriquinone B1, a selective insulin receptor modulator. Chembiochem. 4(5), 379-385 (2003).
[5]. Kim, H., Deng, L., Xiong, X., et al. Glyceraldehyde 3-phosphate dehydrogenase is a cellular target of the insulin mimic demethylasterriquinone B1. J. Med. Chem. 50(15), 3423-3426 (2007).