GSK2578215A

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Cat.No. 4629 - GSK2578215A | C24H18FN3O2 | CAS No. 1285515-21-0
Description: Potent, selective LRRK2 inhibitor; brain penetrant
Chemical Name: 5-(2-Fluoro-4-pyridinyl)-2-(phenylmethoxy)-N-3-pyridinylbenzamide
Purity: ≥99% (HPLC)
Datasheet
Citations (7)
Reviews
Literature

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.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline.

Compound Libraries

GSK2578215A is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 399.42
Formula C24H18FN3O2
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 1285515-21-0
PubChem ID 68107965
InChI Key WCIGMFCFPXZRMQ-UHFFFAOYSA-N
Smiles FC1=NC=CC(C2=CC=C(OCC3=CC=CC=C3)C(C(NC4=CC=CN=C4)=O)=C2)=C1

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 39.94 100

Preparing Stock Solutions

The following data is based on the product molecular weight 399.42. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.5 mL 12.52 mL 25.04 mL
5 mM 0.5 mL 2.5 mL 5.01 mL
10 mM 0.25 mL 1.25 mL 2.5 mL
50 mM 0.05 mL 0.25 mL 0.5 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the biological activity of the product.

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


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Keywords: GSK2578215A, GSK2578215A supplier, leucine, rich, repeat, kinase, 2, LRRK2, inhibitors, inhibits, in, vivo, potent, selective, brain, penetrant, BBB, permeable, parkinsons, parkinson's, 4629, Tocris Bioscience

7 Citations for GSK2578215A

Citations are publications that use Tocris products. Selected citations for GSK2578215A include:

Russo et al (2015) Leucine-rich repeat kinase 2 positively regulates inflammation and down-regulates NF-κB p50 signaling in cultured microglia cells. Oncotarget 12 230 PMID: 26646749

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

Manzoni et al (2013) Inhibition of LRRK2 kinase activity stimulates macroautophagy. Biochim Biophys Acta 1833 2900 PMID: 23916833

Perera et al (2016) Inhibitor treatment of peripheral mononuclear cells from Parkinson's disease patients further validates LRRK2dephosphorylation as a pharmacodynamic biomarker. Scientific Reports 6 31391 PMID: 27503089

Cirnaru et al (2014) LRRK2 kinase activity regulates synaptic vesicle trafficking and neurotransmitter release through modulation of LRRK2 macro-molecular complex. Front Mol Neurosci 7 49 PMID: 24904275

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


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Literature in this Area

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