Bioactivity | DLK-IN-1 is a selective, orally active inhibitor of dual leucine zipper kinase (DLK, MAP3K12), with a Ki of 3 nM. DLK-IN-1 retains excellent CNS penetration and is well tolerated following multiple days of dosing at concentrations that exceed those required for DLK inhibition in the brain. DLK-IN-1 has activity in a model of Alzheimer’s Disease. | |||||||||
Target | Ki: 3 nM (DLK). | |||||||||
Name | DLK-IN-1 | |||||||||
CAS | 1620574-24-4 | |||||||||
Formula | C20H24F3N5O2 | |||||||||
Molar Mass | 423.43 | |||||||||
Appearance | Solid | |||||||||
Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
Storage |
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Reference | [1]. Patel S, et al. Selective Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12) with Activity in a Model of Alzheimer's Disease. J Med Chem. 2017 Oct 12;60(19):8083-8102. |