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  4. GKI-1

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.

GKI-1 Chemical Structure

GKI-1 Chemical Structure

CAS No. : 2444764-03-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 495 In-stock
Solution
10 mM * 1 mL in DMSO USD 495 In-stock
Solid
1 mg USD 180 In-stock
5 mg USD 450 In-stock
10 mg USD 750 In-stock
50 mg   Get quote  
100 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

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Based on 3 publication(s) in Google Scholar

GKI-1 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

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Description

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[1].

IC50 & Target

IC50: 4.9 µM (hGWLFL), 4.9 µM (hGWL-KinDom)[1]
In Vitro

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.

GKI-1 Related Antibodies
Molecular Weight

269.73

Formula

C15H12ClN3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC(C=C1)=CC=C1NC2=CC(C3=CNN=C3)=CC=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7074 mL 18.5371 mL 37.0741 mL
5 mM 0.7415 mL 3.7074 mL 7.4148 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 5 mg/mL (18.54 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: 99.89%

COA (245 KB) LCMS (95 KB)

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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GKI-1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GKI-12444764-03-6GKI1GKI 1OthersInhibitorinhibitorinhibit

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