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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%

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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

Powder: -20°C for 3 years | 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 recommeded.

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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

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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