Home / LRRK2 Inhibitors / GSK2578215A

GSK2578215A

Catalog #: 4629
19 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
4629/25
4629/5
GSK2578215A | CAS No. 1285515-21-0 | LRRK2 Inhibitors
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Description: Potent, selective LRRK2 inhibitor; brain penetrant

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

Purity: ≥99%

Product Details
Citations (19)
Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

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.

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold for research purposes under agreement from GlaxoSmithKline.

Background References

  1. Dysregulation of lysosomal morphology by pathogenic LRRK2 is corrected by TPC2 inhibition.
    Hockey L, Kilpatrick B, Eden E, Lin-Moshier Y, Brailoiu G, Brailoiu E, Futter C, Schapira A, Marchant J, Patel S
    J Cell Sci, 2015;128(2):232-8.
  2. Parkinson disease-associated LRRK2 G2019S transgene disrupts marrow myelopoiesis and peripheral Th17 response
    J Park, JW Lee, SC Cooper, HE Broxmeyer, JR Cannon, CH Kim
    J. Leukoc. Biol., 2017;0(0):.
  3. GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substituent-N-arylbenzamide LRRK2 kinase inhibitor.
    Reith et al.
    Bioorg.Med.Chem.Lett., 2012;22:5625

Product Datasheets

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Citations for GSK2578215A

The citations listed below are publications that use Tocris products. Selected citations for GSK2578215A include:

19 Citations: Showing 1 - 10

  1. LRRK2 is required for CD38-mediated NAADP-Ca2+ signaling and the downstream activation of TFEB (transcription factor EB) in immune cells.
    Authors: Chong-Shan Et al.
    Autophagy  2022;18:204-222
  2. LRRK2 Inhibition Mitigates the Neuroinflammation Caused by TLR2-Specific α-Synuclein and Alleviates Neuroinflammation-Derived Dopaminergic Neuronal Loss.
    Authors: Sung-Woo Et al.
    Cells  2022;11
  3. The small molecule DIPQUO promotes osteogenic differentiation via inhibition of glycogen synthase kinase 3-beta signaling.
    Authors: Shuibing Et al.
    J Biol Chem  2021;296:100696
  4. LRRK2 activation controls the repair of damaged endomembranes in macrophages.
    Authors: Huw R Et al.
    EMBO J  2020;39:e104494
  5. Protein synthesis is suppressed in sporadic and familial Parkinson's disease by LRRK2.
    Authors: Eleanor T Et al.
    FASEB J  2020;34:14217-14233
  6. Leucine-rich repeat kinase 2 phosphorylation on synapsin I regulates glutamate release at pre-synaptic sites.
    Authors: Elisa Et al.
    J Neurochem  2019;150:264-281
  7. Brain injury induces HIF-1α-dependent transcriptional activation of LRRK2 that exacerbates brain damage.
    Authors: Bae Et al.
    Cell Death Dis  2018;9:1125
  8. LRRK2 is a negative regulator of Mycobacterium tuberculosis phagosome maturation in macrophages.
    Authors: Brian D Et al.
    EMBO J  2018;37
  9. LRRK2 impairs autophagy by mediating phosphorylation of leucyl-tRNA synthetase.
    Authors: Ho Et al.
    Cell Biochem Funct  2018;36:431
  10. Leucine-rich repeat kinase 2 controls protein kinase A activation state through phosphodiesterase 4.
    Authors: Russo Et al.
    J Neuroinflammation  2018;15:297
  11. RAB7L1-Mediated Relocalization of LRRK2 to the Golgi Complex Causes Centrosomal Deficits via RAB8A.
    Authors: Madero-Pérez Et al.
    Front Mol Neurosci  2018;11
  12. Inhibitor treatment of peripheral mononuclear cells from Parkinson's disease patients further validates LRRK2dephosphorylation as a pharmacodynamic biomarker.
    Authors: Perera Et al.
    Scientific Reports  2016;6:31391
  13. LRRK2 phosphorylates pre-synaptic N-ethylmaleimide sensitive fusion (NSF) protein enhancing its ATPase activity and SNARE complex disassembling rate.
    Authors: Belluzzi Et al.
    Mol Neurodegener  2016;11:1
  14. Leucine-Rich Repeat Kinase 2 (LRRK2) phosphorylates p53 and induces p21(WAF1/CIP1) expression.
    Authors: Ho Et al.
    Mol Brain  2015;8:54
  15. Leucine-rich repeat kinase 2 modulates neuroinflammation and neurotoxicity in models of human immunodeficiency virus 1-associated neurocognitive disorders.
    Authors: Justin Et al.
    J Neurosci  2015;35:5271-83
  16. Leucine-rich repeat kinase 2 positively regulates inflammation and down-regulates NF-κB p50 signaling in cultured microglia cells.
    Authors: Russo Et al.
    Oncotarget  2015;12:230
  17. LRRK2 kinase activity regulates synaptic vesicle trafficking and neurotransmitter release through modulation of LRRK2 macro-molecular complex.
    Authors: Cirnaru Et al.
    Front Mol Neurosci  2014;7:49
  18. The LRRK2 inhibitor GSK2578215A induces protective autophagy in SH-SY5Y cells: involvement of Drp-1-mediated mitochondrial fission and mitochondrial-derived ROS signaling.
    Authors: Saez-Atienzar Et al.
    Cell Death Dis.  2014;5:e1368
  19. Inhibition of LRRK2 kinase activity stimulates macroautophagy.
    Authors: Manzoni Et al.
    Biochim Biophys Acta  2013;1833:2900

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