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GKI-1
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
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 | Availability | Quantity |
|---|---|---|---|
| 1 mg | $148 | In Stock | |
| 5 mg | $372 | In Stock | |
| 10 mg | $556 | In Stock | |
| 25 mg | $896 | In Stock | |
| 50 mg | $1,220 | In Stock | |
| 100 mg | $1,650 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $397 | In Stock |
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Purity:99.38%
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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.Product Introduction
Bioactivity
Chemical Properties
| 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 | GWL-KinDom (human):4.9 µM , GWLFL (human):4.9 µM , GWLFL (human):4.9 µM, GWL-KinDom (human):2.5 µM, ROCK1:11 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] |
| Molecular Weight | 269.73 |
| Formula | C15H12ClN3 |
| Cas No. | 2444764-03-6 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 180.0 mg/mL (667.3 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Calculator
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 . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (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.
(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 main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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
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