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Description: Gα-protein inhibitor; potent inhibitor of Gq/11 signaling
Chemical Name: (R)-1-((3S,6S,9S,12S,18R,21S,22R)-21-acetamido-18-benzyl-3-((R)-1-methoxyethyl)-4,9,10,12,16,22-hexamethyl-15-methylene-2,5,8,11,14,17,20-heptaoxo-1,19-dioxa-4,7,10,13,16-pentaazacyclodocosan-6-yl)-2-methylpropyl (2S,3R)-2-acetamido-3-hydroxy-4-methylpentanoate
Purity: ≥95% (HPLC)
Biological Activity for YM 254890
YM 254890 is a Gα-protein inhibitor. Potently inhibits Gq/11 heterotrimeric G protein signaling. Inhibits ATP/UTP-induced Ca2+ increase in HCAE cells expressing P2Y2 receptor (IC50 = 50 nM); carbachol-induced production of IP1 in CHO cells expressing M1 receptor (IC50 = 95 nM); and ADP-induced Ca2+ increase in platelets, in vitro (IC50 = 2 μM). Also inhibits Gs-induced cAMP elevation and G protein-coupled MAPK/ERK signaling.
Technical Data for YM 254890
| M. Wt | 960.09 |
| Formula | C46H69N7O15 |
| Storage | Store at -20°C |
| Purity | ≥95% (HPLC) |
| CAS Number | 568580-02-9 |
| PubChem ID | 9919454 |
| InChI Key | QVYLWCAYZGFGNF-WBWCVGBTSA-N |
| Smiles | [H][C@]1(N(C([C@H]([C@@H](C(C)C)OC([C@H]([C@@H](C(C)C)O)NC(C)=O)=O)NC([C@@H](N(C([C@@H](NC(C(N(C([C@H](OC([C@H]([C@H](OC1=O)C)NC(C)=O)=O)CC2=CC=CC=C2)=O)C)=C)=O)C)=O)C)C)=O)=O)C)[C@H](OC)C |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for YM 254890
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 9.6 | 10 |
Preparing Stock Solutions for YM 254890
The following data is based on the product molecular weight 960.09. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 10.42 mL | 52.08 mL | 104.16 mL |
| 0.5 mM | 2.08 mL | 10.42 mL | 20.83 mL |
| 1 mM | 1.04 mL | 5.21 mL | 10.42 mL |
| 5 mM | 0.21 mL | 1.04 mL | 2.08 mL |
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Product Datasheets for YM 254890
References for YM 254890
References are publications that support the biological activity of the product.
Uemura et al (2006) Biological properties of a specific Gα; q/11 inhibitor, YM-254890, on platelet functions and thrombus formation under high-shear stress. Br.J.Pharmacol. 148 61 PMID: 16520742
Xiong et al (2016) Total synthesis and structure-activity relationship studies of a series of selective G protein inhibitors. Nat.Chem. 8 1035 PMID: 27768111
Xiong et al (2019) Structure-activity relationship studies of the natural product Gq/11 protein inhibitor YM-254890. Chem.Med.Chem. 14 865 PMID: 30790465
Peng et al (2021) Functional evidence for biased inhibition of G protein signaling by YM-254890 in human coronary artery endothelial cells. Eur.J.Pharmacol. 891 173706 PMID: 33152337
Schlegel et al (2021) Macrocyclic Gq protein inhibitors FR900359 and/or YM-254890-fit for translation? ACS Pharmacol.Transl.Sci. 4 888 PMID: 33860209
If you know of a relevant reference for YM 254890, please let us know.
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Keywords: YM 254890, YM 254890 supplier, YM254890, heterotrimeric, g, protein, signaling, GPCRs, coupled, receptors, Galpha, Ga, Galfa, G9/11, Gi/o, potent, inhibitors, inhibits, Heterotrimeric, G-protein, GTPases, 7352, Tocris Bioscience
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