AdipoGen Life Sciences


CHF 250.00
In stock
AG-CN2-0509-MC05500 µgCHF 250.00
AG-CN2-0509-M0011 mgCHF 460.00
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Product Details
Synonyms QS 3666A
Product Type Chemical


MW 960.1
CAS 568580-02-9
Source/Host Chemicals Isolated from Chromobacterium sp. QS3666 strain.
Purity Chemicals ≥95% (HPLC)
Appearance Off-white solid.
Solubility Soluble in DMSO (10mg/ml).
Identity Determined by 1H-NMR.
Declaration Not sold in Japan
Smiles O=C(N(C)C(C(N[C@H](C(N(C)[C@H](C(N[C@@H]([C@@H](C(C)C)OC([C@@H](NC(C)=O)[C@@H](C(C)C)O)=O)C1=O)=O)C)=O)C)=O)=C)[C@H](OC([C@@H](NC(C)=O)[C@@H](C)OC([C@@H](N1C)[C@@H](C)OC)=O)=O)CC2=CC=CC=C2
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.
MSDS Download PDF
Product Specification Sheet
Datasheet Download PDF
  • Cyclic depsipeptide composed of unique amino acids differing from normal amino acids.
  • Membrane permeable, potent and selective Gαq family inhibitor. Acts in both in vivo and in vitro systems.
  • 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. Structure of YM-254890, a Novel Gq/11 Inhibitor from Chromobacterium sp. QS3666: M. Taniguchi, et al.; Tetrahedron 59, 4533 (2003)
  2. YM-254890, a novel platelet aggregation inhibitor produced by Chromobacterium sp. QS3666: M. Taniguchi, et al.; J. Antibiot. 56, 358 (2003)
  3. A novel Galphaq/11-selective inhibitor: J. Takasaki, et al.; J. Biol. Chem. 279, 47438 (2004)
  4. 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)
  5. 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)
  6. Structural basis for the specific inhibition of heterotrimeric Gq protein by a small molecule: A. Nishimura, et al.; PNAS 107, 13666 (2010)
  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. 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)
  10. The Gq signalling pathway inhibits brown and beige adipose tissue: K. Klepac, et al.; Nat. Commun. 7, 10895 (2016)
  11. Gaq proteins: molecular pharmacology and therapeutic potential: D. Kamato, et al.; Cell. Mol. Life Sci. 74, 1379 (2017) (Review)
  12. Functional characterization of uveal melanoma oncogenes: J. Ma, et al.; Oncogene, ahead of print (2020)
  13. Exploring pharmacological inhibition of G q/11 as an analgesic strategy: S. Marwari, et al.; Br. J. Pharmacol. ahead of print (2022)
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