Cat. No. Name Size Price Add Cart
KI2553GSK2578215A10 mg$517.4
GSK2578215A50 mg$2197

Chemical Characteristic

Product NameGSK2578215A
SynonymsN/A
CAS No.1285515-21-0
Molecular Weight 399.42
FormulaC24H18FN3O2
Chemical Name2-(benzyloxy)-5-(2-fluoropyridin-4-yl)-N-(pyridin-3-yl)benzamide
SmilesC(=O)(c1c(ccc(c1)c1cc(ncc1)F)OCc1ccccc1)Nc1cnccc1
Chemical Structure

Biological activities

GSK2578215A is a potent and highly selective leucine-rich repeat kinase 2 (LRRK2) inhibitor. GSK2578215A inhibits wild-type LRRK2 and LRRK2G2019S with IC50s of 10.9 and 8.9 nM, respectively. GSK2578215A induces dose-dependent Ser910 and Ser935 dephosphorylation of endogenous LRRK2 in mouse Swiss 3T3 cells.[1] GSK2578215A significantly reduces the increase in growth hormone (GH) extracellular level due to LRRK2G2019S expression.[2]

Protocols

In vitro, GSK2578215A is dissolved in DMSO.[3]

References

[1] Reith AD, et al. GSK2578215A, a potent and highly selective 2-arylmethyloxy- 5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor. Bioorg Med Chem Lett. 2012, 22 (17): 5625-5629.
[2] R Migheli, et al. LRRK2 affects vesicle trafficking, neurotransmitter extracellular level and membrane receptor localization. PLOS ONE. 2013, 8(10): e77198.
[3] Manzoni C, et al. Inhibition of LRRK2 kinase activity stimulates macroautophagy. Biochim Biophys Acta. 2013, 1833 (12): 2900-2910.

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