YM-254890

Off-white solid. Soluble in DMSO (10mg/ml). Cyclic depsipeptide composed of unique amino acids differing from normal amino acids, Membrane permeable, potent and selective Galphaq family inhibitor, Inhibits the signal transduction of Galphaq, Galpha11 and Galpha14 (IC50=0.095&mu,M) by blocking the exchange of GDP for GTP, preventing the activation of the G protein, Inhibits platelet aggregation induced by ADP, Shown to inhibit Galphaq-coupled GPCR signaling by inhibiting calcium mobilization and to have antithrombotic and thrombolytic effects, Might be used as a starting point for new approaches in cancer drug discovery, Galphaq signaling has been shown to regulate brown/beige adipocytes using the structurally similar specific Galphaq family inhibitor FR900359. It is suggested that inhibition of this pathway may be a novel therapeutic approach to combat obesity, The closely related compounds YM-254890 and FR900359 (UBO-QIC) are both potent and selective Galphaq family inhibitors and were for long time only restricted accessible. The commercial availablilty of YM-254890 might give further insights into Galphaq family singaling processes.