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Safety Information

SML3637

Sigma-Aldrich

YM-254890

≥95% (HPLC)

Synonym(s):

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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About This Item

Empirical Formula (Hill Notation):
C46H69N7O15
CAS Number:
568580-02-9
Molecular Weight:
960.08
MDL number:
MFCD09832722
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

Assay

≥95% (HPLC)

form

(Powder or Lyophilized powder or film)

color

white to off-white

storage temp.

-10 to -25°C

Biochem/physiol Actions

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.

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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Certificates of Analysis (COA)

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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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