YM-254890

YM-254890 is a **macrocyclic depsipeptide** that acts as a highly selective inhibitor of the **Gq/11 subfamily of heterotrimeric G proteins**[4][1][5][9][10]. It is a natural product originally isolated from the bacterium Chromobacterium sp. QS3666[9][10]. YM-254890 inhibits Gq protein signaling by binding to the α subunit (Gαq), preventing GDP release and subsequent GTP exchange, thereby arresting signal transduction downstream of G protein-coupled receptors (GPCRs)[4][5][8]. Recent studies report that YM-254890 may also exhibit "biased inhibition" of other G protein pathways, such as Gαs and Gαi/o, especially in MAPK signaling, though its primary mechanism is blockage of Gq/11-driven GPCR signaling[3][8]. YM-254890 is primarily used as a **research tool compound** in cell signaling studies and has not been approved for clinical use as a pharmaceutical. Its physicochemical characteristics include high chemical stability but very low oral bioavailability and brain penetration[1]. It is valuable in research for dissecting G protein signaling in diseases linked to Gq signaling, including potential applications in asthma, inflammation, and cancer models[1][4][6].

Brand names

YM-254890YM254890YM 254890

Other names

YM-254890YM254890YM 254890