YM-254890

Product description: Chemical. CAS: 568580-02-9. Formula: C46H69N7O15. MW: 960.1. 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=0.095µM) 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.

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