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GKI-1

Name: GKI-1
Brand: TargetMol
SKU: T11402
Price: 89 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T11402Cas No. 2444764-03-6

GKI-1 is a Greatwall (GWL) kinase inhibitor with an IC50 of 4.9 for hGWLFL and 2.5 µM for hGWL-KinDom. It exhibits stronger inhibition on ROCK1 with an IC50 of 11 µM and only weakly inhibits PKA.

GKI-1

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Purity: 99.96%

Catalog No. T11402Cas No. 2444764-03-6

GKI-1 is a Greatwall (GWL) kinase inhibitor with an IC50 of 4.9 for hGWLFL and 2.5 µM for hGWL-KinDom. It exhibits stronger inhibition on ROCK1 with an IC50 of 11 µM and only weakly inhibits PKA.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$89	In Stock	In Stock
5 mg	$223	In Stock	In Stock
10 mg	$333	In Stock	In Stock
25 mg	$538	In Stock	In Stock
50 mg	$732	In Stock	In Stock
100 mg	$990	-	In Stock
1 mL x 10 mM (in DMSO)	$238	In Stock	In Stock

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

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.96%

Appearance:Solid

Color:White

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	GKI-1 is a Greatwall (GWL) kinase inhibitor with an IC50 of 4.9 for hGWLFL and 2.5 µM for hGWL-KinDom. It exhibits stronger inhibition on ROCK1 with an IC50 of 11 µM and only weakly inhibits PKA.
Targets&IC50	GWLFL (human):4.9 µM, ROCK1:11 µM, GWL-KinDom (human):4.9 µM , GWLFL (human):4.9 µM , GWL-KinDom (human):2.5 µM
In vitro	Treatment of HeLa cells with GKI-1 (25 and 50µM, 0-8.5 h) reduced ENSA/ARPP19 phosphorylation levels, resulting in reduced mitotic events, mitotic arrest/cell death, and cell division failure. GKI-1 inhibited full-length human GWL and showed cellular effects[1]

Chemical Properties

Molecular Weight	269.73
Formula	C₁₅H₁₂ClN₃
Cas No.	2444764-03-6
Smiles	N(C=1C=C(C=CC1)C=2C=NNC2)C3=CC=C(Cl)C=C3
Relative Density.	1.320 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: 180 mg/mL (667.33 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (18.54 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	3.7074 mL	18.5371 mL	37.0741 mL	185.3706 mL
5 mM	0.7415 mL	3.7074 mL	7.4148 mL	37.0741 mL
10 mM	0.3707 mL	1.8537 mL	3.7074 mL	18.5371 mL
20 mM	0.1854 mL	0.9269 mL	1.8537 mL	9.2685 mL
50 mM	0.0741 mL	0.3707 mL	0.7415 mL	3.7074 mL
100 mM	0.0371 mL	0.1854 mL	0.3707 mL	1.8537 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