YM 254890

Name: YM 254890
Brand: Tocris Bioscience
SKU: 7352

Tocris Bioscience, part of Bio-Techne | Catalog # 7352

Citations (11)

COA / SDS

Gα-protein inhibitor; potent inhibitor of Gq/11 signaling

Key Product Details

Description:	Gα-protein inhibitor; potent inhibitor of G_q/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)
Molecular Weight:	960.09

View Full Technical Details for YM 254890

Technical Data
Citations

Biological Activity for YM 254890

YM 254890 is a G_α-protein inhibitor. Potently inhibits G_q/11 heterotrimeric G protein signaling. Inhibits ATP/UTP-induced Ca²⁺ increase in HCAE cells expressing P2Y₂receptor (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 G_s-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 for YM 254890

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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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References for YM 254890

References are publications that support the biological activity of the product.

Schlegel Macrocyclic G_q 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 G_q/11 protein inhibitor YM-254890. Chem.Med.Chem. 2019 PMID: 30790465
Uemura Biological properties of a specific G_α q/11 inhibitor, YM-254890, on platelet functions and thrombus formation under high-shear stress. Br.J.Pharmacol. 2006 PMID: 16520742