GKI-1
Based on 3 publication(s) in Google Scholar
GKI-1 is a Greatwall (GWL) kinase inhibitor with IC50s of 4.9 and 2.5 μM against hGWLFL and hGWL-KinDom, respectively. GKI-1 robustly inhibits ROCK1 with an IC50 of 11 μM, but only weakly affected PKA.
For research use only. We do not sell to patients.
- Purity: 99.96%
- CAS No.: 2444764-03-6
- Formula: C15H12ClN3
- Molecular Weight:269.73
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Storage:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) GKI-1
More
Biological Activity
IC50: 4.9 µM (hGWLFL), 4.9 µM (hGWL-KinDom)[1]
GKI-1 inhibits full-length human GWL, and shows cellular efficacy[1].
Treatment of HeLa cells (25 and 50 μM, 0-8.5 hours) with GKI-1 reduces ENSA/ARPP19 phosphorylation levels, resulting in a decrease in mitotic events, mitotic arrest/cell death and cytokinesis failure[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2444764-03-6
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Appearance Solid
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Molecular Weight 269.73
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Formula C15H12ClN3
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Color White to off-white
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SMILES
ClC(C=C1)=CC=C1NC2=CC(C3=CNN=C3)=CC=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (3)
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Journal Impact Factor
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Most Recent
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Cell Rep Med
Harnessing transcriptionally driven chromosomal instability adaptation to target therapy-refractory lethal prostate cancer. [Abstract]2023 Feb 21;4(2):100937. PMID: 36787737 -
iScience
MASTL is enriched in cancerous and pluripotent stem cells and influences OCT1/OCT4 levels. [Abstract]2022 May 25;25(6):104459. PMID: 35677646 -
Sci Rep
2022 Jun 22;12(1):10568. PMID: 35732702
Solvent & Solubility
DMSO : 200 mg/mL (741.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (18.54 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.17 mg/mL (8.05 mM); Clear solution
This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.7074 mL | 18.5371 mL | 37.0741 mL | 92.6853 mL |
| 5 mM | 0.7415 mL | 3.7074 mL | 7.4148 mL | 18.5371 mL | |
| 10 mM | 0.3707 mL | 1.8537 mL | 3.7074 mL | 9.2685 mL | |
| 15 mM | 0.2472 mL | 1.2358 mL | 2.4716 mL | 6.1790 mL | |
| 20 mM | 0.1854 mL | 0.9269 mL | 1.8537 mL | 4.6343 mL | |
| 25 mM | 0.1483 mL | 0.7415 mL | 1.4830 mL | 3.7074 mL | |
| 30 mM | 0.1236 mL | 0.6179 mL | 1.2358 mL | 3.0895 mL | |
| 40 mM | 0.0927 mL | 0.4634 mL | 0.9269 mL | 2.3171 mL | |
| 50 mM | 0.0741 mL | 0.3707 mL | 0.7415 mL | 1.8537 mL | |
| 60 mM | 0.0618 mL | 0.3090 mL | 0.6179 mL | 1.5448 mL | |
| 80 mM | 0.0463 mL | 0.2317 mL | 0.4634 mL | 1.1586 mL | |
| 100 mM | 0.0371 mL | 0.1854 mL | 0.3707 mL | 0.9269 mL |
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