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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

🥰Excellent

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. However, due to objective factors, there is a small probability that the synthesis may not be successful during the R&D process. We appreciate your understanding. If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

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Purity:99.96%

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COA HNMR LCMS

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	ROCK1:11 µM, GWLFL (human):4.9 µM , GWLFL (human):4.9 µM, GWL-KinDom (human):2.5 µM, GWL-KinDom (human):4.9 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: 180.0 mg/mL (667.3 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 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

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