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Hetrotrimeric Gq proteins specific inhibitor

YM-254890 is a cyclic depsipeptide isolated from a soil bacterium Chromobacterium sp. QS3666 strain and has a cyclic peptide structure composed of unique amino acids differing from normal amino acids.   It specifically inhibits signals mediated by Gq, G11 and G14, which are Gq family of heterotrimeric G proteins and are involved in elevated Ca2+ level among about 20 types of G proteins, by acting on GDP/GTP exchange reaction.  It is a first membrane permeable compound particularly inhibiting Gq signal and a useful tool for a study analyzing Gq signals.

Leaflet Package insert

1. Features

  • Specifically inhibits signals mediated by Gαq, Gα11, and Gα14
  • Low-moleclar membrane permeable compound
  • Acts in both in vivo and in vitro systems

2. Basic information

  • Structure formula
  • CAS No. 568580-02-9
  • Assay: >95% (HPLC)
  • How to use: Dissolve it in DMSO at 1-10 mmol/L to prepare stock solution*.
    In use, acccordingly dilute it with an experimental solution.
    *: Go through the stock solution as soon as possible.

3. References

  1. Nishimura, A. et al., "Structural basis for the specific inhibition of heterotrimeric Gq protein by a small molecule.", PNAS, 107(31), 13666-13671 (2010).
  2. Takasaki, J. et al., "A novel Gαq/11-selective inhibitor.", J. Biol. Chem., 279(46), 47438-47445 (2004)
  3. Taniguchi, M. et al., "Structure of YM-254890, a novel Gq/11 inhibitor from Chromobacterium sp. QS3666.", Tetrahedron, 59, 4533-4538 (2003).
  4. Taniguchi, M. et al., "YM-254890, a novel platelet aggregation inhibitor produced by Chromobacterium sp. QS3666.", J. Antibiotics, 56(4), 358-363 (2003).

4. Product List

Product Name Package Size Wako Cat. No. Storage Condition
1 mg
Keep at 2-10°C.
10 mg

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