tcsc2482 Dorsomorphin (dihydrochloride)

Dorsomorphin dihydrochloride is a potent and selective AMPK inhibitor, that is competitive with ATP, with K_i of 109±16 nM in the absence of AMP.

IC50 & Target: Ki: 109±16 nM (AMPK)^[1]

In Vitro: HT1080 cells are treated with 10 μM Dorsomorphin for 2 h under 2DG stress. Immunoblot analysis reveals that phosphorylation levels of the catalytic α subunit of AMPK are increased by exposure of HT1080 cells to 2DG, whereas both basal and 2DG-induced phosphorylation levels are clearly reduced when Dorsomorphin is added. Measurements of cellular kinase activity using an ELISA-based assay system confirmed that Dorsomorphin does reduce the endogenous AMPK activity regardless of cell culture conditions^[2].

In Vivo: Administration of Dorsomorphin over 24 h leads to a 60% increase in total serum iron concentrations. Dorsomorphin treatment is therefore effective in reducing basal levels of hepcidin expression and increasing serum iron concentrations in adult mice^[3].