Cat. No. 4629
Chemical Name: 5-(2-Fluoro-4-pyridinyl)-2-(phenylm
Biological ActivityPotent 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 InformationSold for research purposes under agreement from GlaxoSmithKline.
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 / Safety Data Sheet
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.
Ho et al (2015) Leucine-Rich Repeat Kinase 2 (LRRK2) phosphorylates p53 and induces p21(WAF1/CIP1) expression. Mol Brain 8 54. PMID: 26384650.
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.
View Related Products by Target
View Related Products by Product Action
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
Find multiple products by catalog number
New Products in this Area
Potent Nek2 inhibitorRoscovitine
Potent, selective cyclin-dependent kinase inhibitorEnzastaurin
Potent PKCβ inhibitorBMS 265246
Potent cdk1/2 inhibitorAutocamtide-2-related inhibitory peptide, myristoylated
CaM kinase II inhibitor; enhanced cell permeable derivative of Autocamtide-2-related inhibitory peptideMP A08
Selective ATP competitive SphK1 and 2 inhibitor; cell permeableAkti-1/2
Potent and selective dual Akt1 and 2 inhibitorVX 680
High affinity and selective Aurora kinase inhibitorImatinib mesylate
Potent and selective v-Abl tyrosine kinase inhibitor; also inhibits PDGFR and c-kitTGX 221
Potent and selective PI 3-kinase β inhibitorPF 543 hydrochloride
Potent and selective SphK1 inhibitorJX 06
Potent and selective pyruvate dehydrogenase kinase (PDK) 1/2/3 inhibitorMRT 68601 hydrochloride
Potent TBK1 inhibitorAzoramide
Unfolded protein response (UPR) modulator
Follow Tocris on LinkedIn
Visit our LinkedIn page for the latest Tocris news, events and updates.