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GKI-1 

Cat. No.: HY-100521 Purity: 99.25%
Handling Instructions

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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 495 In-stock
Estimated Time of Arrival: December 31
5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 750 In-stock
Estimated Time of Arrival: December 31
100 mg Get quote
250 mg Get quote
500 mg Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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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].

Molecular Weight

269.73

Formula

C₁₅H₁₂ClN₃

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)

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
10 mM 0.3707 mL 1.8537 mL 3.7074 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References

Purity: 99.25%

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Keywords:

GKI-1GKI1GKI 1OthersInhibitorinhibitorinhibit

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Product name:
GKI-1
Cat. No.:
HY-100521
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