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CZC-25146 is a selective and cell-penetrant inhibitor of leucine-rich repeat kinase-2 (LRRK2) with IC50 value of 4.76nM [1].

CZC-25146 is a second generation inhibitor of LRRK2 with excellent potency and selectivity. In a time-resolved fluorescence resonance energy transfer assay, CZC-25146 shows potent inhibition of both recombinant human wild type LRRK2 and G2019S mutant LRRK2 with IC50 values of 4.76nM and 6.87nM, respectively. CZC-25146 is selective against LRRK2. When treated with 184 different protein kinases and one lipid kinase, CZC-25146 inhibits only five of them with high potency including PLK4, GAK, TNK1, CAMKK2 and PIP4K2C. Besides that, CZC-25146 is found to relieve the G2019S LRRK2-induced cell injury and death with EC50 value of 100nM in neurons of primary rodent cortical. It also attenuates G2019S LRRK2-induced human neuronal injury with EC50 value of 4nM. However, CZC-25146 lacks sufficient brain exposure to be used in rodent models of PD [1, 2].

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