GSK2578215A

Potent, selective LRRK2 inhibitor; brain penetrant CAS# 1285515-21-0

GSK2578215A

Catalog No. BCC6243----Order now to get a substantial discount!

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GSK2578215A: 5mg $35 In Stock
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Quality Control of GSK2578215A

Number of papers citing our products

Chemical structure

GSK2578215A

3D structure

Chemical Properties of GSK2578215A

Cas No. 1285515-21-0 SDF Download SDF
PubChem ID 68107965 Appearance Powder
Formula C24H18FN3O2 M.Wt 399.42
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 50 mg/mL (125.18 mM; Need ultrasonic)
Chemical Name 5-(2-fluoropyridin-4-yl)-2-phenylmethoxy-N-pyridin-3-ylbenzamide
SMILES C1=CC=C(C=C1)COC2=C(C=C(C=C2)C3=CC(=NC=C3)F)C(=O)NC4=CN=CC=C4
Standard InChIKey WCIGMFCFPXZRMQ-UHFFFAOYSA-N
Standard InChI InChI=1S/C24H18FN3O2/c25-23-14-19(10-12-27-23)18-8-9-22(30-16-17-5-2-1-3-6-17)21(13-18)24(29)28-20-7-4-11-26-15-20/h1-15H,16H2,(H,28,29)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of GSK2578215A

DescriptionPotent 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.

GSK2578215A Dilution Calculator

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GSK2578215A Molarity Calculator

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Preparing Stock Solutions of GSK2578215A

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.5036 mL 12.5182 mL 25.0363 mL 50.0726 mL 62.5908 mL
5 mM 0.5007 mL 2.5036 mL 5.0073 mL 10.0145 mL 12.5182 mL
10 mM 0.2504 mL 1.2518 mL 2.5036 mL 5.0073 mL 6.2591 mL
50 mM 0.0501 mL 0.2504 mL 0.5007 mL 1.0015 mL 1.2518 mL
100 mM 0.025 mL 0.1252 mL 0.2504 mL 0.5007 mL 0.6259 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on GSK2578215A

GSK2578215A is a potent and highly selective LRRK2 inhibitor; exhibits IC50s of around 10 nM against both wild-type LRRK2 and the G2019S mutant. IC50 value: ~10 nM(wt-LRRK2; LRRK2 G2019S) [1] Target: LRRK2 inhibitor GSK2578215A exhibits exceptionally high selectivity for LRRK2 across the kinome, substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant at a concentration of 0.3–1.0 μM in cells and in mouse spleen and kidney, but not in brain, following intraperitoneal injection of 100 mg/kg [1].

References:
[1]. Reith AD, et al. GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor. Bioorg Med Chem Lett. 2012 Sep 1;22(17):5625-9.

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References on GSK2578215A

The LRRK2 inhibitor GSK2578215A induces protective autophagy in SH-SY5Y cells: involvement of Drp-1-mediated mitochondrial fission and mitochondrial-derived ROS signaling.[Pubmed:25118928]

Cell Death Dis. 2014 Aug 14;5:e1368.

Mutations in the leucine-rich repeat kinase 2 (LRRK2) gene have been associated with Parkinson's disease, and its inhibition opens potential new therapeutic options. Among the drug inhibitors of both wild-type and mutant LRRK2 forms is the 2-arylmethyloxy-5-subtitutent-N-arylbenzamide GSK257815A. Using the well-established dopaminergic cell culture model SH-SY5Y, we have investigated the effects of GSK2578215A on crucial neurodegenerative features such as mitochondrial dynamics and autophagy. GSK2578215A induces mitochondrial fragmentation of an early step preceding autophagy. This increase in autophagosome results from inhibition of fusion rather than increases in synthesis. The observed effects were shared with LRRK2-IN-1, a well-described, structurally distinct kinase inhibitor compound or when knocking down LRRK2 expression using siRNA. Studies using the drug mitochondrial division inhibitor 1 indicated that translocation of the dynamin-related protein-1 has a relevant role in this process. In addition, autophagic inhibitors revealed the participation of autophagy as a cytoprotective response by removing damaged mitochondria. GSK2578215A induced oxidative stress as evidenced by the accumulation of 4-hydroxy-2-nonenal in SH-SY5Y cells. The mitochondrial-targeted reactive oxygen species scavenger MitoQ positioned these species as second messengers between mitochondrial morphologic alterations and autophagy. Altogether, our results demonstrated the relevance of LRRK2 in mitochondrial-activated pathways mediating in autophagy and cell fate, crucial features in neurodegenerative diseases.

GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor.[Pubmed:22863203]

Bioorg Med Chem Lett. 2012 Sep 1;22(17):5625-9.

Leucine-rich repeat kinase 2 (LRRK2) is a promising therapeutic target for some forms of Parkinson's disease. Here we report the discovery and characterization of 2-arylmethyloxy-5-subtitutent-N-arylbenzamides with potent LRRK2 activities exemplified by GSK2578215A which exhibits biochemical IC(50)s of around 10 nM against both wild-type LRRK2 and the G2019S mutant. GSK2578215A exhibits exceptionally high selectivity for LRRK2 across the kinome, substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant at a concentration of 0.3-1.0 muM in cells and in mouse spleen and kidney, but not in brain, following intraperitoneal injection of 100mg/kg.

Description

GSK2578215A is a potent and highly selective LRRK2 inhibitor, which exhibits IC50s of around 10 nM against both wild-type LRRK2 and the G2019S mutant.

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