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YM-254890

AG-CN2-0509-MC05 500 µg INQ
AG-CN2-0509-M001 1 mg INQ
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Additional Information

Product Data
Synonyms QS 3666A
Properties
Formula C46H69N7O15
MW 960.1
CAS 568580-02-9
Source/Host Isolated from Chromobacterium sp. QS3666 strain.
Purity ≥95% (HPLC)
Appearance Off-white solid.
Solubility Soluble in DMSO (10mg/ml).
Origin Not sold in Japan
InChi Key QVYLWCAYZGFGNF-WBWCVGBTSA-N
Product Type Chemical
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Handling Advice Keep cool and dry.
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
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Product Description

  • Cyclic depsipeptide composed of unique amino acids differing from normal amino acids.
  • Membrane permeable, potent and selective Gαq family inhibitor.
  • Inhibits the signal transduction of Gαq, Gα11 and Gα14 (IC50=0.095μM) by blocking the exchange of GDP for GTP, preventing the activation of the G protein.
  • Inhibits platelet aggregation induced by ADP.
  • Shown to inhibit Gαq-coupled GPCR signaling by inhibiting calcium mobilization and to have antithrombotic and thrombolytic effects.
  • Might be used as a starting point for new approaches in cancer drug discovery.
  • q signaling has been shown to regulate brown/beige adipocytes using the structurally similar specific Gαq family inhibitor FR900359. It is suggested that inhibition of this pathway may be a novel therapeutic approach to combat obesity.
  • The closely related compounds YM-254890 and FR900359 (UBO-QIC) are both potent and selective Gαq family inhibitors and were for long time only restricted accessible. The commercial availability of YM-254890 might give further insights into Gαq family signaling processes.

Product References

  1. YM-254890, a novel platelet aggregation inhibitor produced by Chromobacterium sp. QS3666: M. Taniguchi, et al.; J. Antibiot. 56, 358 (2003)
  2. A novel Galphaq/11-selective inhibitor: J. Takasaki, et al.; J. Biol. Chem. 279, 47438 (2004)
  3. Pharmacological properties of YM-254890, a specific G(alpha)q/11 inhibitor, on thrombosis and neointima formation in mice: T. Kawasaki, et al.; Thromb. Haemost. 94, 184 (2005)
  4. Effect of YM-254890, a specific G(alpha)q/11 inhibitor, on experimental peripheral arterial disease in rats: T. Uemura, et al.; Eur. J. Pharmacol. 536, 154 (2006)
  5. Structural basis for the specific inhibition of heterotrimeric Gq protein by a small molecule: A. Nishimura, et al.; PNAS 107, 13666 (2010)
  6. Total synthesis and structure-activity relationship studies of a series of selective G protein inhibitors: X.F. Xiong, et al.; Nat. Chem. 8, 1035 (2016)
  7. Structure, Function, Pharmacology, and Therapeutic Potential of the G Protein, Gα/q,11: D. Kamato, et al.; Front. Cardiovasc. Med. 2, 14 (2015) (Review)
  8. Total synthesis of the cyclic depsipeptide YM-280193, a platelet aggregation inhibitor: H. Kaur, et al.; Org. Lett. 17, 492 (2015)
  9. Gaq proteins: molecular pharmacology and therapeutic potential: D. Kamato, et al.; Cell. Mol. Life Sci. (Epub ahead of print) (2016) (Review)
  10. The Gq signalling pathway inhibits brown and beige adipose tissue: K. Klepac, et al.; Nat. Commun. 7, 10895 (2016)
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