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ARUK2010489

🥰Excellent
Catalog No. T212596
Alias ARUK-2010489, ARUK2010489, ARUK 2010489

ARUK2010489 (Compound 23) is a potent, selective, and brain-penetrant NUAK1 inhibitor with a pIC50 of 8.7, also exhibiting partial inhibitory activity against CDK2, CDK4, and CDK6 at micromolar concentrations, and it is applied in neurological disease research, including mechanistic studies related to Alzheimer’s disease.

ARUK2010489

ARUK2010489

🥰Excellent
Catalog No. T212596Alias ARUK-2010489, ARUK2010489, ARUK 2010489
ARUK2010489 (Compound 23) is a potent, selective, and brain-penetrant NUAK1 inhibitor with a pIC50 of 8.7, also exhibiting partial inhibitory activity against CDK2, CDK4, and CDK6 at micromolar concentrations, and it is applied in neurological disease research, including mechanistic studies related to Alzheimer’s disease.
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Product Introduction

Bioactivity
Description
ARUK2010489 (Compound 23) is a potent, selective, and brain-penetrant NUAK1 inhibitor with a pIC50 of 8.7, also exhibiting partial inhibitory activity against CDK2, CDK4, and CDK6 at micromolar concentrations, and it is applied in neurological disease research, including mechanistic studies related to Alzheimer’s disease.
Targets&IC50
CDK6:3.84 μM, NUAK1:8.7nM, CDK2:14.28 μM, CDK4:2.56 μM
In vitro
Method: Optimization of the CDK2 inhibitor NU6140 was performed to generate selective NUAK1 inhibitors, followed by pharmacokinetic and brain penetration studies in mice.
Result: ARUK2010694 showed improved plasma half-life, while ARUK2010489 demonstrated high brain penetration (mouse Kp,u,ub = 2.29) and selective NUAK1 inhibition without CDK2 activity[1].
SynonymsARUK-2010489, ARUK2010489, ARUK 2010489
Chemical Properties
Molecular Weight404.55
FormulaC24H32N6
SmilesCC(C)N1CCN(C2=CC=C(NC3=NC(CCC4CC4)=C(C=CN5)C5=N3)C=C2)CC1
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2OTargetMol | reagent mix well and clarify
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