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GSK2578215A

Chemical Structure GSK2578215A

CAS No.: 1285515-21-0

GSK2578215A (GSK-2578215A)

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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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; shows 8-fold reduced potentcy against A2016T mutant LRRK2 (IC50=81 nM); 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; induces protective autophagy in SH-SY5Y cells.

Physicochemical Properties

M.Wt 399.417
Formula C24H18FN3O2
CAS No. 1285515-21-0
Storage
Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 3 Month
Shipping
Solubility

10 mM in DMSO

Chemical Name

Benzamide, 5-(2-fluoro-4-pyridinyl)-2-(phenylmethoxy)-N-3-pyridinyl-

Clinical Information

References

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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