GSK2578215A

Catalog # Availability Size / Price Qty
4629/25
4629/5
LRRK2 Inhibitors Small Molecule
1 Image
Description: Potent, selective LRRK2 inhibitor; brain penetrant

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

Purity: ≥99%

Product Details
Citations (10)
Reviews

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.

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.

Product Datasheets

Reconstitution Calculator
Molarity Calculator

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Molarity Calculator

=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Citations for GSK2578215A

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

10 Citations: Showing 1 - 10

  1. Brain injury induces HIF-1α-dependent transcriptional activation of LRRK2 that exacerbates brain damage.
    Authors: Bae Et al.
    Cell Death Dis  2018;9:1125
  2. Leucine-rich repeat kinase 2 controls protein kinase A activation state through phosphodiesterase 4.
    Authors: Russo Et al.
    J Neuroinflammation  2018;15:297
  3. RAB7L1-Mediated Relocalization of LRRK2 to the Golgi Complex Causes Centrosomal Deficits via RAB8A.
    Authors: Madero-Pérez Et al.
    Front Mol Neurosci  2018;11
  4. 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
  5. 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
  6. Leucine-Rich Repeat Kinase 2 (LRRK2) phosphorylates p53 and induces p21(WAF1/CIP1) expression.
    Authors: Ho Et al.
    Mol Brain  2015;8:54
  7. 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
  8. 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
  9. 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
  10. Inhibition of LRRK2 kinase activity stimulates macroautophagy.
    Authors: Manzoni Et al.
    Biochim Biophys Acta  2013;1833:2900

FAQs

No product specific FAQs exist for this product, however you may

View all Small Molecule FAQs

Reviews for GSK2578215A

There are currently no reviews for this product. Be the first to review GSK2578215A and earn rewards!

Have you used GSK2578215A?

Submit a review and receive an Amazon gift card.

$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review
Tocris Bioscience is the leading supplier of novel and exclusive tools for life science research with over 30 years' experience in the industry. Tocris is a Bio-Techne brand.