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GeA-69

Name: GeA-69
Brand: TargetMol
SKU: T5399
Price: 35 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T5399Cas No. 2143475-98-1

GeA-69 (GeA69) is a selective and allosteric PARP14 macrodomain 2 (MD2) inhibitor (Kd: 0.86 μM in ITC assays).

GeA-69

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Purity: 99.85%

Catalog No. T5399Cas No. 2143475-98-1

GeA-69 (GeA69) is a selective and allosteric PARP14 macrodomain 2 (MD2) inhibitor (Kd: 0.86 μM in ITC assays).

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$35	In Stock	In Stock
10 mg	$58	In Stock	In Stock
25 mg	$118	In Stock	In Stock
50 mg	$208	In Stock	In Stock
100 mg	$287	In Stock	In Stock
200 mg	$418	-	In Stock
1 mL x 10 mM (in DMSO)	$37	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:99.85%

Appearance:Solid

Color:White

Resource Download

COA HNMR LCMS

Product Introduction

Bioactivity

Description	GeA-69 (GeA69) is a selective and allosteric PARP14 macrodomain 2 (MD2) inhibitor (Kd: 0.86 μM in ITC assays).
Targets&IC50	PARP14:0.86 μM (Kd, in ITC assays)
In vitro	The macrodomain recruitment was significantly decreased in cells pre-treated with 50 μM GeA-69 and completely prevented in cells exposed to 250 μM GeA-69.
Kinase Assay	Binding experiments were carried out on a VP-ITC microcalorimeter. All experiments were performed in 50 mM HEPES (pH 7.4), 300 mM NaCl, 5 % glycerol, 0.5 mM TCEP at 12 °C, a reference power of 12 μCal/sec and a stirring speed of 307 rpm. The titrations were conducted using an initial injection of 2 μL followed by 28 identical injections of 10 μL with duration of 4 sec (per injection) and a spacing of 240 sec between injections. Competition experiments were performed on an iTC200 instrument at 20 °C, a reference power of 12 μCal/sec and a stirring speed of 1000 rpm. Following an initial injection of 0.2 μL, 20 identical injections of 2 μL were run with a duration of 4 sec (per injection) and a spacing of 150 sec between injections. Data analysis was carried out using Origin software with the MicroCal plugin. Thermodynamic parameters were calculated using ΔG = ΔH ? TΔS = ?RTlnKB, where ΔG, ΔH, and ΔS are the changes in free energy, enthalpy, and entropy of binding, respectively. In all cases, a single binding site model was employed.

Chemical Properties

Molecular Weight	300.35
Formula	C₂₀H₁₆N₂O
Cas No.	2143475-98-1
Smiles	CC(=O)Nc1ccccc1-c1cccc2c3ccccc3[nH]c12
Relative Density.	1.281 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: 120 mg/mL (399.53 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (13.32 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	3.3294 mL	16.6472 mL	33.2945 mL	166.4724 mL
5 mM	0.6659 mL	3.3294 mL	6.6589 mL	33.2945 mL
10 mM	0.3329 mL	1.6647 mL	3.3294 mL	16.6472 mL
20 mM	0.1665 mL	0.8324 mL	1.6647 mL	8.3236 mL
50 mM	0.0666 mL	0.3329 mL	0.6659 mL	3.3294 mL
100 mM	0.0333 mL	0.1665 mL	0.3329 mL	1.6647 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