AG-CN2-0509-MC05500 µgCHF 250.00
AG-CN2-0509-M0011 mgCHF 460.00
|Source/Host Chemicals||Isolated from Chromobacterium sp. QS3666 strain.|
|Purity Chemicals||≥95% (HPLC)|
|Solubility||Soluble in DMSO (10mg/ml).|
|Declaration||Not sold in Japan|
|Shipping and Handling|
|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.|
|Product Specification Sheet|
- 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.
- Gαq 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.
- YM-254890, a novel platelet aggregation inhibitor produced by Chromobacterium sp. QS3666: M. Taniguchi, et al.; J. Antibiot. 56, 358 (2003)
- A novel Galphaq/11-selective inhibitor: J. Takasaki, et al.; J. Biol. Chem. 279, 47438 (2004)
- 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)
- 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)
- Structural basis for the specific inhibition of heterotrimeric Gq protein by a small molecule: A. Nishimura, et al.; PNAS 107, 13666 (2010)
- 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)
- Structure, Function, Pharmacology, and Therapeutic Potential of the G Protein, Gα/q,11: D. Kamato, et al.; Front. Cardiovasc. Med. 2, 14 (2015) (Review)
- Total synthesis of the cyclic depsipeptide YM-280193, a platelet aggregation inhibitor: H. Kaur, et al.; Org. Lett. 17, 492 (2015)
- Gaq proteins: molecular pharmacology and therapeutic potential: D. Kamato, et al.; Cell. Mol. Life Sci. (Epub ahead of print) (2016) (Review)
- The Gq signalling pathway inhibits brown and beige adipose tissue: K. Klepac, et al.; Nat. Commun. 7, 10895 (2016)