SML3637
YM-254890
≥95% (HPLC)
别名:
N-Acetyl-L-threonyl-(aR)-a-hydroxybenzenepropanoyl-2,3-didehydro-N-methylalanyl-L-alanyl-N-methyl-L-alanyl-(3R)-3-[[(2S,3R)-2-(acetylamino)-3-hydroxy-4-methyl-1-oxopentyl]oxy]-L-leucyl-N,O-dimethyl-L-threonine (7→1)-lactone, QS 3666A, YM 254890
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生化／生理作用
YM-254890, a cyclic depsipeptide isolated from the culture broth of Chromobacterium sp., is a cell-permeable, potent and selective inhibitor of Gαq/11 protein. YM-254890 specifically inhibits the GDP/GTP exchange by blocking GDP release from the Gq protein.
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
Akiyuki Nishimura et al.
Proceedings of the National Academy of Sciences of the United States of America, 107(31), 13666-13671 (2010-07-20)
Heterotrimeric GTP-binding proteins (G proteins) transmit extracellular stimuli perceived by G protein-coupled receptors (GPCRs) to intracellular signaling cascades. Hundreds of GPCRs exist in humans and are the targets of a large percentage of the pharmaceutical drugs used today. Because G
Markus Kuschak et al.
British journal of pharmacology, 177(8), 1898-1916 (2019-12-28)
G proteins are intracellular switches that transduce and amplify extracellular signals from GPCRs. The Gq protein subtypes, which are coupled to PLC activation, can act as oncogenes, and their expression was reported to be up-regulated in cancer and inflammatory diseases.
Jun Takasaki et al.
The Journal of biological chemistry, 279(46), 47438-47445 (2004-09-02)
YM-254890, which was isolated from the culture broth of Chromobacterium sp., inhibits ADP-induced platelet aggregation and has antithrombotic and thrombolytic effects. YM-254890 blocks Galpha(q/11)-coupled ADP receptor P2Y1-mediated Ca(2+) mobilization. Here we report that YM-254890 is a selective Galpha(q/11) inhibitor. YM-254890
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