GSK2578215A

Cat. No. 4629

GSK2578215A C24H18FN3O2 [1285515-21-0]

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Chemical Name: 5-(2-Fluoro-4-pyridinyl)-2-(phenylmethoxy)-N-3-pyridinylbenzamide

Biological Activity

Potent LRRK2 inhibitor (IC50 values are 8.9 and 10.1 nM for LRRK2[G2019S] mutant and wild-type LRRK2 respectively). Displays selectivity for LRRK2 over a panel of 460 other kinases. Blocks Ser910 and Ser935 phosphorylation in vitro and in peripheral tissues in vivo. Brain penetrant.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline.

Technical Data

M.Wt:
399.42
Formula:
C24H18FN3O2
Solubility:
Soluble to 100 mM in DMSO
Purity:
>99 %
Storage:
Store at RT
CAS No:
1285515-21-0

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

Reith et al (2012) GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substituent-N-arylbenzamide LRRK2 kinase inhibitor. Bioorg.Med.Chem.Lett. 22 5625. PMID: 22863203.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for GSK2578215A include:

Belluzzi et al (2016) LRRK2 phosphorylates pre-synaptic N-ethylmaleimide sensitive fusion (NSF) protein enhancing its ATPase activity and SNARE complex disassembling rate. Mol Neurodegener 11 1. PMID: 26758690.

Perera et al (2016) Inhibitor treatment of peripheral mononuclear cells from Parkinson's disease patients further validates LRRK2dephosphorylation as a pharmacodynamic biomarker. Scientific Reports 6 31391. PMID: 27503089.

Ho et al (2015) Leucine-Rich Repeat Kinase 2 (LRRK2) phosphorylates p53 and induces p21(WAF1/CIP1) expression. Mol Brain 8 54. PMID: 26384650.

Russo et al (2015) Leucine-rich repeat kinase 2 positively regulates inflammation and down-regulates NF-κB p50 signaling in cultured microglia cells. Oncotarget 12 230. PMID: 26646749.

Saez-Atienzar et al (2014) The LRRK2 inhibitor GSK2578215A induces protective autophagy in SH-SY5Y cells: involvement of Drp-1-mediated mitochondrial fission and mitochondrial-derived ROS signaling. Cell Death Dis. 5 e1368. PMID: 25118928.

Manzoni et al (2013) Inhibition of LRRK2 kinase activity stimulates macroautophagy. Biochim Biophys Acta 1833 2900. PMID: 23916833.

Do you know of a great paper that uses GSK2578215A from Tocris? If so please let us know.show all ▼show less ▲

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Keywords: GSK2578215A, supplier, leucine, rich, repeat, kinase, 2, LRRK2, inhibitors, inhibits, in, vivo, potent, selective, brain, penetrant, BBB, permeable, parkinsons, parkinson's, Tocris Bioscience, LRRK2 Inhibitor products

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