JH-II-127 is an orally available, brain penetrant, potent and selective inhibitor of both wild-type and G2019S mutant Leucine-rich repeat kinase 2 (LRRK2). JH-II-127 inhibits phosphorylation of the Ser910 and Ser935 of both wild-type and G2019S mutant LRRK2. It causes complete inhibition of LRRK2 in mouse brain at 100 mg/kg.
orally available, brain penetrant, potent and selective inhibitor of both wild-type and G2019S mutant Leucine-rich repeat kinase 2 (LRRK2)
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11 - Combustible Solids
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WGK 3
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Not applicable
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Not applicable
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Activating mutations in leucine-rich repeat kinase 2 (LRRK2) are present in a subset of Parkinson's disease (PD) patients and may represent an attractive therapeutic target. Here we report a 2-anilino-4-methylamino-5-chloropyrrolopyrimidine, JH-II-127 (18), as a potent and selective inhibitor of both
Clinical pharmacology : advances and applications, 8, 177-189 (2016-11-02)
Major advances in understanding how genetics underlies Parkinson's disease (PD) have provided new opportunities for understanding disease pathogenesis and potential new targets for therapeutic intervention. One such target is leucine-rich repeat kinase 2 (LRRK2), an enigmatic enzyme implicated in both
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