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A-395

Name: A-395
Brand: TargetMol
SKU: T10205
Price: 218 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T10205Cas No. 2089148-72-9

A-395 is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12, IC50: 18 nM).

A-395

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Purity: 98.43%

Catalog No. T10205Cas No. 2089148-72-9

A-395 is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12, IC50: 18 nM).

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$40	In Stock	In Stock
5 mg	$89	In Stock	In Stock
10 mg	$132	In Stock	In Stock
25 mg	$218	In Stock	In Stock
50 mg	Preferential	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$95	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:98.43%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	A-395 is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12, IC50: 18 nM).
Targets&IC50	PRC2:18 nM
In vitro	The embryonic ectoderm development (EED) protein is an essential subunit of PRC2. A-395 antagonizes the H3K27me3 binding functions of EED by binding to the H3K27me3-binding pocket, thereby preventing the allosteric activation of PRC2's catalytic activity. A-395 competes for H3K27me3 peptide binding to EED (IC50: 7 nM) and selectively modulates PRC2 activity in cells, markedly reducing the H3K27 methyl mark. A-395 inhibits H3K27me2 and H3K27me3 (IC50s: 390 nM and 90 nM, respectively) and induces growth inhibition in human tumor cell lines sensitive to SAM-competitive EZH2 inhibitors, unlike its close chemical analog A-395N.
Cell Research	1,000 multiple myeloma cells are seeded in each well of 96-well cell culture plates and treated with A-395 (0.001-100 μM) or DMSO control for 10 d before the cell proliferation assay. Cell proliferation assays are conducted with the CellTiter-Glo Luminescent Cell Viability Assay.

Chemical Properties

Molecular Weight	486.65
Formula	C₂₆H₃₅FN₄O₂S
Cas No.	2089148-72-9
Smiles	CN(C)[C@H]1CN(C[C@@H]1c1ccc(cc1)N1CCN(CC1)S(C)(=O)=O)C1CCc2cccc(F)c12
Relative Density.	1.30 g/cm3 (Predicted)

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 100 mg/mL (205.49 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 1 mg/mL (2.05 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	2.0549 mL	10.2743 mL	20.5486 mL	102.7432 mL
5 mM	0.4110 mL	2.0549 mL	4.1097 mL	20.5486 mL
10 mM	0.2055 mL	1.0274 mL	2.0549 mL	10.2743 mL
20 mM	0.1027 mL	0.5137 mL	1.0274 mL	5.1372 mL
50 mM	0.0411 mL	0.2055 mL	0.4110 mL	2.0549 mL
100 mM	0.0205 mL	0.1027 mL	0.2055 mL	1.0274 mL

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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