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GAK inhibitor 49 

Cat. No.: HY-124793
Handling Instructions

GAK inhibitor 49 is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with a Ki of 0.54 nM and a cell IC50 of 56 nM. GAK inhibitor 49 also shows binding to RIPK2.

For research use only. We do not sell to patients.

GAK inhibitor 49 Chemical Structure

GAK inhibitor 49 Chemical Structure

CAS No. : 319492-82-5

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Description

GAK inhibitor 49 is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with a Ki of 0.54 nM and a cell IC50 of 56 nM. GAK inhibitor 49 also shows binding to RIPK2[1].

In Vitro

GAK inhibitor 49 (compound 49) shows a weak inhibitory effect on AAK1, BMP2K and STK16, with IC50s of 28, 63 and >100μM, respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

370.40

Formula

C₂₀H₂₂N₂O₅

CAS No.

319492-82-5

SMILES

COC1=C(OC)C(OC)=CC(NC2=CC=NC3=CC(OC)=C(OC)C=C23)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (134.99 mM; ultrasonic and warming and heat to 80°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6998 mL 13.4989 mL 26.9978 mL
5 mM 0.5400 mL 2.6998 mL 5.3996 mL
10 mM 0.2700 mL 1.3499 mL 2.6998 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: ≥ 2.5 mg/mL (6.75 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.75 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (6.75 mM); Clear solution

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

GAK inhibitor 49GAK inhibitor49GAK inhibitor-49OthersATP-competitiveselectiveNAKfamilyInhibitorinhibitorinhibit

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GAK inhibitor 49
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HY-124793
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