Trimeric G Protein Gq Family-specific Inhibitor

YM-254890

This compound is a cyclic depsipeptide isolated from the soil bacterium Chromobacterium QS3666 strain.

Among the Gq family of trimeric G proteins, it specifically inhibits signals mediated through Gαq, Gα11, and Gα14 (among about 20 varieties of G protein, those involved in increasing Ca ion concentration) by acting on the GDP/GTP exchange reaction.

This compound is the first membrane-permeable compound that selectively inhibits Gq signals, and will become a useful tool in Gq signal analysis studies.

Features
Basic Information
Structural formula
References
Product List
Related Information

Features

Specifically inhibits signals mediated through Gαq, Gα11, and Gα14
Membrane-permeable, low-molecular-weight compound
Acts in both in vivo and in vitro systems

Basic Information

○ CAS RN^® 568580-02-9

○ Purity：　≥ 95.0 %

○ How to use：　Dissolve in DMSO to a concentration of 1 to 10 mmol/L to make a stock solution. Prior to use, dilute appropriately with the solution of the experimental system.

*Stock solutions should be used as soon as possible.

Structural formula

References

1) Nishimura, A. et al. : Proc. Natl. Acad. Sci. USA, 107(31), 13666 (2010). Structural basis for the specific inhibition of heterotrimeric G_q protein by a small molecule

2) Takasaki, J. et al. : J. Biol. Chem., 279(46), 47438 (2004). A Novel Gα_q/11-selective Inhibitor

3) Taniguchi, M. et al. : Tetrahedron, 59(25), 4533 (2003). Structure of YM-254890, a Novel G_q/11 Inhibitor from Chromobacterium sp. QS3666

4) Taniguchi, M. et al. : J. Antibiotics, 56(4), 358 (2003). YM-254890, a Novel Platelet Aggregation Inhibitor Produced by Chromobacterium sp. QS3666.",

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For research use or further manufacturing use only. Not for use in diagnostic procedures.

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