Chemical Structure : GSK2578215A
CAS No.: 1285515-21-0
Catalog No.: PC-43416Not For Human Use, Lab Use Only.
GSK2578215A is a highly potent, selective, BBB-permeable LRRK2 inhibitor with IC50 of 10.9 and 9.9 nM for wild-type LRRK2 and the G2019S mutant, respectively.
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GSK2578215A is a highly potent, selective, BBB-permeable LRRK2 inhibitor with IC50 of 10.9 and 9.9 nM for wild-type LRRK2 and the G2019S mutant, respectively.
GSK2578215A shows 8-fold reduced potentcy against A2016T mutant LRRK2 (IC50=81 nM).
GSK2578215A inhibits Ser910 and Ser935 phosphorylation in both wild-type LRRK2 and LRRK2 G2019S stably transfected into HEK293 cells at 0.1-0.3 uM, also induces dephosphorylation of Ser910 and 935 at 1-3 μM in the inhibitor-resistant LRRK2[A2016T+ G2019S] and LRRK2 [A2016T] mutants.
GSK2578215A induces protective autophagy in SH-SY5Y cells.
M.Wt | 399.417 | |
Formula | C24H18FN3O2 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
Benzamide, 5-(2-fluoro-4-pyridinyl)-2-(phenylmethoxy)-N-3-pyridinyl- |
1. Reith AD, et al. Bioorg Med Chem Lett. 2012 Sep 1;22(17):5625-9.
2. Saez-Atienzar S, et al. Cell Death Dis. 2014 Aug 14;5:e1368.
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