Chemical Structure : KAI-11101
CAS No.:
KAI-11101
Catalog No.: PC-23614Not For Human Use, Lab Use Only.
KAI-11101 is a potent, selective, brain-penetrant dual leucine zipper kinase (DLK, MAP3K12) inhibitor with Ki of 0.7 nM and cellular p-JNK IC50 of 51 nM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
KAI-11101 is a potent, selective, brain-penetrant dual leucine zipper kinase (DLK, MAP3K12) inhibitor with Ki of 0.7 nM and cellular p-JNK IC50 of 51 nM.
KAI-11101 shows inhibition of paclitaxel-induced MAPK pathway activation through reduction of phosphorylated cJun (p-cJun; IC50 = 95 nM) in ex vivo DRG CIPN assay, also demonstrates phenotypic protection against paclitaxel-induced axon degeneration (EC50 = 363 nM).
KAI-11101 displayed an excellent in vitro safety profile and showed neuroprotective properties in an ex vivo axon fragmentation assay as well as dose-dependent activity in a mouse PD model.
Physicochemical Properties
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M.Wt
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469.44
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Formula
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C21H23F4N5O3
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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3-(6-Amino-5-(difluoromethoxy)pyridin-3-yl)-6-((1R,2S)-4,4-difluoro-2-methoxy cyclohexyl)-1-ethyl-1,6-dihydro-7H-pyrazolo[3,4-c]pyridin-7-one
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References
1. Lagiakos HR, et al. J Med Chem. 2024 Dec 13. doi: 10.1021/acs.jmedchem.4c02074.
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