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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.


| 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]. |
| Synonyms | ARUK-2010489, ARUK2010489, ARUK 2010489 |
| Molecular Weight | 404.55 |
| Formula | C24H32N6 |
| Smiles | CC(C)N1CCN(C2=CC=C(NC3=NC(CCC4CC4)=C(C=CN5)C5=N3)C=C2)CC1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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