KAI-11101

Chemical Structure : KAI-11101

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货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	469.44
分子式	C21H23F4N5O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	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

参考文献

1. Lagiakos HR, et al. J Med Chem. 2024 Dec 13. doi: 10.1021/acs.jmedchem.4c02074.

KAI-11101

生物&药学活性

物理化学性质&存储条件

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KAI-11101

生物&药学活性

物理化学性质&存储条件

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