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Description

A cell-permeable, orally bioavailable, blood-brain barrier permeant 2,6-diaminopyridine based compound that acts as a highly potent and selective inhibitor of dual leucine zipper kinase inhibitor (DLK, Ki = 500 pM). Exhibits an ideal balance of metabolic stability, potency, and efflux properties. Displays high selectivity over JNK (IC = 129, 514, and 364 nM for JNK1, 2, and 3, respectively) and MLK (IC = 67.8, 767, and 602 nM for MLK1, 2, and 3, respectively). Does not affect the activities of MKK4 and MKK7 (IC >5 microM). Protects neurons in an in vitro axon degeneration assay (IC = 107 nM). Also shown to reduce levels of phosphorylated c-Jun in retina and offer protection in a 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MTPT) model of Parkinson&prime,s disease. Exhibits desirable pharmacokinetic properties (t1/2 = 0.6 h, CLp = 56 ml/min/kg in mice, 1 mg/kg, i.v., or 5 mg/kg, p.o.).Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water., A cell-permeable, orally bioavailable, blood-brain barrier permeant 2,6-diaminopyridine based compound that acts as a highly potent and selective inhibitor of dual leucine zipper kinase inhibitor (DLK, Ki = 500 pM). Exhibits an ideal balance of metabolic stability, potency, and efflux properties. Displays high selectivity over JNK (IC = 129, 514, and 364 nM for JNK1, 2, and 3, respectively) and MLK (IC = 67.8, 767, and 602 nM for MLK1, 2, and 3, respectively). Does not affect the activities of MKK4 and MKK7 (IC >5 microM). Protects neurons in an in vitro axon degeneration assay (IC = 107 nM). Also shown to reduce levels of phosphorylated c-Jun in retina and offer protection in a 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MTPT) model of Parkinson&prime,s disease. Exhibits desirable pharmacokinetic properties (t1/2 = 0.6 h, CLp = 56 ml/min/kg in mice, 1 mg/kg, i.v., or 5 mg/kg, p.o.).