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YM-254890

Name: YM-254890
Brand: TargetMol
SKU: T17273
Rating: 4.5 (1 reviews)

(Synonyms: YM254890, YM 254890) Copy Product Info

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Synonyms: YM254890, YM 254890

Catalog No. T17273 Copy Product Info

Purity: 95%

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YM-254890 (YM) is a natural product and a Gαq/11 protein inhibitor (IC50 < 0.6 μM) with high selectivity and cell permeability. YM-254890 inhibits ADP-induced platelet aggregation by blocking the P2Y1 signaling pathway, and is widely used in research on thrombosis, pain, and uveal melanoma.

Cas No. 568580-02-9

Pack Size	Price	USA Stock	Global Stock	Quantity
1 mg	$1,107	35 days	35 days

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:95%

Appearance:Solid

Color:White

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Product Introduction

Bioactivity

Description	YM-254890 (YM) is a natural product and a Gαq/11 protein inhibitor (IC50 < 0.6 μM) with high selectivity and cell permeability. YM-254890 inhibits ADP-induced platelet aggregation by blocking the P2Y1 signaling pathway, and is widely used in research on thrombosis, pain, and uveal melanoma.
Targets & IC50	HL-60 cells:> 10 μM, P2Y2-C6-15 cells:0.15 μM
In vitro	Methods: Gαiq98,238 mutant protein and HEK293 cells were used, with single-molecule FRET, nucleotide exchange assays, and fluorescent reporter gene assays performed at YM-254890 concentrations of 0.02–200 μM, with incubation times of 20 min–18 h. Results: YM-254890 stabilized the closed conformation of the G protein domain, inhibited GDP release and nucleotide loading, reduced Gq-mediated reporter gene expression, and showed inhibitory effects on both mutant and wild-type proteins. [1] Methods: HEK293, HEK293 αq/11 KO, and HeLa cells were used, incubated with 1 μM YM-254890 for 1 h to 24 h, to perform immunofluorescence, pERK detection, dual-luciferase reporter, protein pull-down, and co-immunoprecipitation experiments. Results: YM-254890 induced translocation of αqQ209L from the cell membrane to the cytoplasm, inhibited its signal transduction, showed no inhibitory effect on membrane-localization-restricted αqQ209L mutants, and could bind to αq and regulate its protein interactions. [2]
Synonyms	YM254890, YM 254890

Chemical Properties

Molecular Weight	960.08
Formula	C₄₆H₆₉N₇O₁₅
Cas No.	568580-02-9
Smiles	CO[C@H](C)[C@@H]1N(C)C(=O)[C@@H](NC(=O)[C@H](C)N(C)C(=O)[C@H](C)NC(=O)C(=C)N(C)C(=O)[C@@H](Cc2ccccc2)OC(=O)[C@@H](NC(C)=O)[C@@H](C)OC1=O)[C@H](OC(=O)[C@@H](NC(C)=O)[C@H](O)C(C)C)C(C)C
Relative Density.	1.26 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 30 mg/mL (31.25 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 1.5 mg/mL (1.56 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.0416 mL	5.2079 mL	10.4158 mL	52.0790 mL
5 mM	0.2083 mL	1.0416 mL	2.0832 mL	10.4158 mL
10 mM	0.1042 mL	0.5208 mL	1.0416 mL	5.2079 mL
20 mM	0.0521 mL	0.2604 mL	0.5208 mL	2.6039 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc