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A-366

Name: A-366
Brand: TargetMol
SKU: T3624
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T3624Cas No. 1527503-11-2

Alias A366, A 366

A-366 is a highly selective peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP, respectively.It is more than 1,000-fold selective for G9a and GLP over the other 21 methyltransferases. It is an inhibitor of the Spindlin1-H3K4me3 interaction with an IC50 of 182.6 nM.It exhibits high affinity for human H3R with a Ki value of 17 nM, and shows subtype selectivity between subgroups of the histaminergic and dopaminergic receptor families.

A-366

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Purity: 99.8%

Catalog No. T3624Alias A366, A 366Cas No. 1527503-11-2

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$30	-	In Stock
2 mg	$43	-	In Stock
5 mg	$68	In Stock	In Stock
10 mg	$92	In Stock	In Stock
25 mg	$219	-	In Stock
50 mg	$378	Inquiry	Inquiry
100 mg	$558	Inquiry	Inquiry
1 mL x 10 mM (in DMSO)	$75	-	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:99.8%

Color:Yellow

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Product Introduction

Bioactivity

Description	A-366 is a highly selective peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP, respectively.It is more than 1,000-fold selective for G9a and GLP over the other 21 methyltransferases. It is an inhibitor of the Spindlin1-H3K4me3 interaction with an IC50 of 182.6 nM.It exhibits high affinity for human H3R with a Ki value of 17 nM, and shows subtype selectivity between subgroups of the histaminergic and dopaminergic receptor families.
Targets&IC50	G9a/GLP:3.3 nM
In vitro	For tumor cell growth, A-366 had less toxic effects than some other G9a/GLP small molecule compound inhibitors, and no difference in the methylation effect on H3K9me2. Various leukemia cell lines were treated with A-366 in vitro, and these tumor cells would produce significant differentiation and morphological changes.
In vivo	For tumor cell growth, A-366 had less toxic effects than some other G9a/GLP small molecule compound inhibitors, and no difference in the methylation effect on H3K9me2. Various leukemia cell lines were treated with A-366 in vitro, and these tumor cells would produce significant differentiation and morphological changes.
Kinase Assay	7.5× compounds are added to a 96-well PolyPlate containing 60 μL of Buffer per well with substrates CoA (200 μM), ATP (400 μM), and [14C]citrate. Reaction is started with 4 μL (300 ng/well) ACL, and the plate is incubated at 37°C for 3 h. Th
Cell Research	PC-3 prostate adenocarcinoma cells are incubated in triplicate with DMSO or the indicated concentrations of A-366 or UNC0638 for 72 hours. H3K9me2 levels are assessed by In-Cell Western assay. (Only for Reference)
Synonyms	A366, A 366

Chemical Properties

Molecular Weight	329.44
Formula	C₁₉H₂₇N₃O₂
Cas No.	1527503-11-2
Smiles	COc1cc2c(cc1OCCCN1CCCC1)N=C(N)C21CCC1
Relative Density.	1.29 g/cm3 (Predicted)

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 32.9 mg/mL (99.87 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.07 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	3.0355 mL	15.1773 mL	30.3545 mL	151.7727 mL
5 mM	0.6071 mL	3.0355 mL	6.0709 mL	30.3545 mL
10 mM	0.3035 mL	1.5177 mL	3.0355 mL	15.1773 mL
20 mM	0.1518 mL	0.7589 mL	1.5177 mL	7.5886 mL
50 mM	0.0607 mL	0.3035 mL	0.6071 mL	3.0355 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