YM-254890

Cyclic depsipeptide composed of unique amino acids differing from normal amino acids.
Membrane permeable, potent and selective Gαq family inhibitor. Acts in both in vivo and in vitro systems.
Inhibits the signal transduction of Gαq, Gα11 and Gα14 (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 Gαq-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.
Gαq signaling has been shown to regulate brown/beige adipocytes using the structurally similar specific Gαq 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 Gαq family inhibitors and were for long time only restricted accessible. The commercial availability of YM-254890 might give further insights into Gαq family signaling processes.