YM 254890
Tocris Bioscience, part of Bio-Techne | Catalog # 7352
Gα-protein inhibitor; potent inhibitor of Gq/11 signaling
Key Product Details
Description
Gα-protein inhibitor; potent inhibitor of Gq/11 signaling
Product Description
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.Product Specifications
Molecular Weight
960.09
Formula
C46H69N7O15
Storage
Store at -20°C
Purity
≥95% (HPLC)
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
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.
Solubility
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Schlegel Macrocyclic Gq protein inhibitors FR900359 and/or YM-254890-fit for translation? ACS Pharmacol.Transl.Sci. 2021 PMID: 33860209
- Peng Functional evidence for biased inhibition of G protein signaling by YM-254890 in human coronary artery endothelial cells. Eur.J.Pharmacol. 2021 PMID: 33152337
- Xiong Total synthesis and structure-activity relationship studies of a series of selective G protein inhibitors. Nat.Chem. 2016 PMID: 27768111
- Xiong Structure-activity relationship studies of the natural product Gq/11 protein inhibitor YM-254890. Chem.Med.Chem. 2019 PMID: 30790465
- Uemura Biological properties of a specific Gα q/11 inhibitor, YM-254890, on platelet functions and thrombus formation under high-shear stress. Br.J.Pharmacol. 2006 PMID: 16520742
Product Specific Notices for YM 254890
For research use only
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