GSK2578215A

Pricing Availability   Qty
Description: Potent, selective LRRK2 inhibitor; brain penetrant
Chemical Name: 5-(2-Fluoro-4-pyridinyl)-2-(phenylmethoxy)-N-3-pyridinylbenzamide
Purity: ≥99% (HPLC)
Datasheet
Citations (19)
Reviews
Literature (1)

Biological Activity for GSK2578215A

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.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline.

Compound Libraries for GSK2578215A

GSK2578215A is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for GSK2578215A

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.

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

Solubility Data for GSK2578215A

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

Preparing Stock Solutions for GSK2578215A

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

Select a batch to recalculate based on the batch molecular weight:
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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References for GSK2578215A

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

19 Citations for GSK2578215A

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

Bae et al (2018) Brain injury induces HIF-1α-dependent transcriptional activation of LRRK2 that exacerbates brain damage. Cell Death Dis 9 1125 PMID: 30420654

Madero-Pérez et al (2018) RAB7L1-Mediated Relocalization of LRRK2 to the Golgi Complex Causes Centrosomal Deficits via RAB8A. Front Mol Neurosci 11 PMID: 30483055

Russo et al (2018) Leucine-rich repeat kinase 2 controls protein kinase A activation state through phosphodiesterase 4. J Neuroinflammation 15 297 PMID: 30368241

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

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

Shuibing et al (2021) The small molecule DIPQUO promotes osteogenic differentiation via inhibition of glycogen synthase kinase 3-beta signaling. J Biol Chem 296 100696 PMID: 33895139

Justin et al (2015) Leucine-rich repeat kinase 2 modulates neuroinflammation and neurotoxicity in models of human immunodeficiency virus 1-associated neurocognitive disorders. J Neurosci 35 5271-83 PMID: 25834052

Brian D et al (2018) LRRK2 is a negative regulator of Mycobacterium tuberculosis phagosome maturation in macrophages. EMBO J 37 PMID: 29789389

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

Chong-Shan et al (2022) LRRK2 is required for CD38-mediated NAADP-Ca2+ signaling and the downstream activation of TFEB (transcription factor EB) in immune cells. Autophagy 18 204-222 PMID: 34313548

Sung-Woo et al (2022) LRRK2 Inhibition Mitigates the Neuroinflammation Caused by TLR2-Specific α-Synuclein and Alleviates Neuroinflammation-Derived Dopaminergic Neuronal Loss. Cells 11 PMID: 35269482

Elisa et al (2019) Leucine-rich repeat kinase 2 phosphorylation on synapsin I regulates glutamate release at pre-synaptic sites. J Neurochem 150 264-281 PMID: 31148170

Ho et al (2018) LRRK2 impairs autophagy by mediating phosphorylation of leucyl-tRNA synthetase. Cell Biochem Funct 36 431 PMID: 30411383

Huw R et al (2020) LRRK2 activation controls the repair of damaged endomembranes in macrophages. EMBO J 39 e104494 PMID: 32643832

Eleanor T et al (2020) Protein synthesis is suppressed in sporadic and familial Parkinson's disease by LRRK2. FASEB J 34 14217-14233 PMID: 32926469

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


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