product summary
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company name :
Tocris Bioscience
product type :
chemical
product name :
4629/5
catalog :
4629/5
quantity :
5 mg (also 25 mg)
price :
173 USD
more info or order :
citations: 21
Reference
Ho D, Nam D, Seo M, Park S, Seol W, Son I. LRRK2 Inhibition Mitigates the Neuroinflammation Caused by TLR2-Specific α-Synuclein and Alleviates Neuroinflammation-Derived Dopaminergic Neuronal Loss. Cells. 2022;11: pubmed publisher
Nabar N, Heijjer C, Shi C, Hwang I, Ganesan S, Karlsson M, et al. LRRK2 is required for CD38-mediated NAADP-Ca2+ signaling and the downstream activation of TFEB (transcription factor EB) in immune cells. Autophagy. 2021;:1-19 pubmed publisher
Cook B, Walker N, Zhang Q, Chen S, Evans T. The small molecule DIPQUO promotes osteogenic differentiation via inhibition of glycogen synthase kinase 3-beta signaling. J Biol Chem. 2021;296:100696 pubmed publisher
Deshpande P, Flinkman D, Hong Y, Goltseva E, Siino V, Sun L, et al. Protein synthesis is suppressed in sporadic and familial Parkinson's disease by LRRK2. FASEB J. 2020;34:14217-14233 pubmed publisher
Herbst S, Campbell P, Harvey J, Bernard E, Papayannopoulos V, Wood N, et al. LRRK2 activation controls the repair of damaged endomembranes in macrophages. EMBO J. 2020;:e104494 pubmed publisher
Marte A, Russo I, Rebosio C, Valente P, Belluzzi E, Pischedda F, et al. Leucine-rich repeat kinase 2 phosphorylation on synapsin I regulates glutamate release at pre-synaptic sites. J Neurochem. 2019;150:264-281 pubmed publisher
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
Hartlova A, Herbst S, Peltier J, Rodgers A, Bilkei Gorzo O, Fearns A, et al. LRRK2 is a negative regulator of Mycobacterium tuberculosis phagosome maturation in macrophages. EMBO J. 2018;37: pubmed publisher
Park J, Lee J, Cooper S, Broxmeyer H, Cannon J, Kim C. Parkinson disease-associated LRRK2 G2019S transgene disrupts marrow myelopoiesis and peripheral Th17 response. J Leukoc Biol. 2017;102:1093-1102 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-κB 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
Puccini J, Marker D, Fitzgerald T, Barbieri J, Kim C, Miller Rhodes P, et al. Leucine-rich repeat kinase 2 modulates neuroinflammation and neurotoxicity in models of human immunodeficiency virus 1-associated neurocognitive disorders. J Neurosci. 2015;35:5271-83 pubmed publisher
Hockey L, Kilpatrick B, Eden E, Lin Moshier Y, Brailoiu G, Brailoiu E, et al. Dysregulation of lysosomal morphology by pathogenic LRRK2 is corrected by TPC2 inhibition. J Cell Sci. 2015;128:232-8 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
image
image 1 :
Tocris Bioscience 4629/5 image 1
Cat.No. 4629 - GSK2578215A C24H18FN3O2 CAS No. 1285515-21-0
product information
master code :
4629
SKU :
4629/5
product name :
GSK2578215A
unit size :
5 mg (also 25 mg)
description :
Potent, selective LRRK2 inhibitor; brain penetrant
target :
LRRK2 Inhibitors
category :
Small Molecules
purity :
99%
observed molecular weight :
399.42
url print :
?utm_source=labome&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules
details of functionality :
GSK2578215A is a 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.
top caption :
Potent, selective LRRK2 inhibitor; brain penetrant
extended description :
Potent, selective LRRK2 inhibitor; brain penetrant
chemical name text :
5-(2-Fluoro-4-pyridinyl)-2-(phenylmethoxy)-N-3-pyridinylbenzamide
formula :
C24H18FN3O2
formula text :
C24H18FN3O2
cas num :
1285515-21-0
USD :
173 USD
product details :
Potent, selective LRRK2 inhibitor; brain penetrant
storage :
Store at RT
more info or order :
company information
Tocris Bioscience
The Watkins Building
Atlantic Road
Avonmouth, Bristol
BS11 9QD
info@bio-techne.com
https://www.tocris.com
800-343-7475
headquarters: UK