YM 254890
Chemical Name: (R)-1-((3S,6S,9S,12S,18R,21S,22R)-21-acetamido-18-benzyl-3-((R)-1-methoxyethyl)-4,9,10,12,16,22-hexamethyl-15-methylene-2,5,8,11,14,17,20-heptaoxo-1,19-dioxa-4,7,10,13,16-pentaazacyclodocosan-6-yl)-2-methylpropyl (2S,3R)-2-acetamido-3-hydroxy-4-methylpentanoate
Purity: ≥95%
Biological Activity
YM 254890 is a Gα-protein inhibitor. Potently inhibits Gq/11 heterotrimeric G protein signaling. Inhibits ATP/UTP-induced Ca2+ increase in HCAE cells expressing P2Y2 receptor (IC50 = 50 nM); carbachol-induced production of IP1 in CHO cells expressing M1 receptor (IC50 = 95 nM); and ADP-induced Ca2+ increase in platelets, in vitro (IC50 = 2 μM). Also inhibits Gs-induced cAMP elevation and G protein-coupled MAPK/ERK signaling.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Biological properties of a specific Gα; q/11 inhibitor, YM-254890, on platelet functions and thrombus formation under high-shear stress.
Uemura et al.
Br.J.Pharmacol., 2006;148:61 -
Total synthesis and structure-activity relationship studies of a series of selective G protein inhibitors.
Xiong et al.
Nat.Chem., 2016;8:1035 -
Structure-activity relationship studies of the natural product Gq/11 protein inhibitor YM-254890.
Xiong et al.
Chem.Med.Chem., 2019;14:865 -
Functional evidence for biased inhibition of G protein signaling by YM-254890 in human coronary artery endothelial cells.
Peng et al.
Eur.J.Pharmacol., 2021;891:173706
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