GSK2578215A | Tocris Bioscience 4629 product information

product summary

company name :

Tocris Bioscience

product type :

chemical

product name :

GSK2578215A

catalog :

4629

quantity :

25 mg

price :

520 USD

more info or order :

Tocris Bioscience product webpage

citations: 11

Reference
Madero Pérez J, Fernández B, Lara Ordóñez A, Fdez E, Lobbestael E, Baekelandt V, et al. RAB7L1-Mediated Relocalization of LRRK2 to the Golgi Complex Causes Centrosomal Deficits via RAB8A. Front Mol Neurosci. 2018;11:417 pubmed publisher
Bae Y, Joo H, Bae J, Hyeon S, Her S, Ko E, et al. Brain injury induces HIF-1α-dependent transcriptional activation of LRRK2 that exacerbates brain damage. Cell Death Dis. 2018;9:1125 pubmed publisher
Ho D, Kim H, Nam D, Sim H, Kim J, Kim H, et al. LRRK2 impairs autophagy by mediating phosphorylation of leucyl-tRNA synthetase. Cell Biochem Funct. 2018;36:431-442 pubmed publisher
Russo I, Di Benedetto G, Kaganovich A, Ding J, Mercatelli D, Morari M, et al. Leucine-rich repeat kinase 2 controls protein kinase A activation state through phosphodiesterase 4. J Neuroinflammation. 2018;15:297 pubmed publisher
Perera G, Ranola M, Rowe D, Halliday G, Dzamko N. Inhibitor treatment of peripheral mononuclear cells from Parkinson's disease patients further validates LRRK2 dephosphorylation as a pharmacodynamic biomarker. Sci Rep. 2016;6:31391 pubmed publisher
Belluzzi E, Gonnelli A, Cirnaru M, Marte A, Plotegher N, Russo I, et al. LRRK2 phosphorylates pre-synaptic N-ethylmaleimide sensitive fusion (NSF) protein enhancing its ATPase activity and SNARE complex disassembling rate. Mol Neurodegener. 2016;11:1 pubmed publisher
Russo I, Berti G, Plotegher N, Bernardo G, Filograna R, Bubacco L, et al. Leucine-rich repeat kinase 2 positively regulates inflammation and down-regulates NF-ÎºB p50 signaling in cultured microglia cells. J Neuroinflammation. 2015;12:230 pubmed publisher
Ho D, Kim H, Kim J, Sim H, Ahn H, Kim J, et al. Leucine-Rich Repeat Kinase 2 (LRRK2) phosphorylates p53 and induces p21(WAF1/CIP1) expression. Mol Brain. 2015;8:54 pubmed publisher
Saez Atienzar S, Bonet Ponce L, Blesa J, Romero F, Murphy M, Jordan J, et al. 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. 2014;5:e1368 pubmed publisher
Cirnaru M, Marte A, Belluzzi E, Russo I, Gabrielli M, Longo F, et al. LRRK2 kinase activity regulates synaptic vesicle trafficking and neurotransmitter release through modulation of LRRK2 macro-molecular complex. Front Mol Neurosci. 2014;7:49 pubmed publisher
Manzoni C, Mamais A, Dihanich S, Abeti R, Soutar M, Plun Favreau H, et al. Inhibition of LRRK2 kinase activity stimulates macroautophagy. Biochim Biophys Acta. 2013;1833:2900-2910 pubmed publisher

product information

brand :

Tocris

master code :

4629

SKU :

4629/25

product name :

GSK2578215A

description :

Potent, selective LRRK2 inhibitor; brain penetrant

target :

LRRK2 Inhibitors

category :

Small Molecules

unit size :

25 mg

purity :

99%

observed molecular weight :

399.42

url print :

?utm_source=distributor&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules

details of functionality :

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.

catalog number base :

4629

product keywords :

leucine rich repeat kinase 2 LRRK2 inhibitors inhibits in vivo potent selective brain penetrant BBB permeable parkinsons parkinson s LRRK2 4629, LRRK 2

extended description :

Potent, selective LRRK2 inhibitor; brain penetrant

chemical name text :

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

formula :

C 24 H 18 FN 3 O 2

formula text :

C24H18FN3O2

cas num :

1285515-21-0

2020 USD :

504

2021 USD :

520 USD

storage :

Store at RT

more info or order :

Tocris Bioscience product webpage