GSK2578215A
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MedKoo CAT#: 406662

CAS#: 1285515-21-0

Description: GSK2578215A is a potent and highly selective LRRK2 kinase inhibitor. GSK2578215A induces protective autophagy in SH-SY5Y cells: involvement of Drp-1-mediated mitochondrial fission and mitochondrial-derived ROS signaling.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. GSK2578215A induces mitochondrial fragmentation of an early step preceding autophagy. GSK2578215A induced oxidative stress as evidenced by the accumulation of 4-hydroxy-2-nonenal in SH-SY5Y cells.


Chemical Structure

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GSK2578215A
CAS# 1285515-21-0

Theoretical Analysis

MedKoo Cat#: 406662
Name: GSK2578215A
CAS#: 1285515-21-0
Chemical Formula: C24H18FN3O2
Exact Mass: 399.13831
Molecular Weight: 399.43
Elemental Analysis: C, 72.17; H, 4.54; F, 4.76; N, 10.52; O, 8.01

Price and Availability

Size Price Availability Quantity
25.0mg USD 150.0 2 Weeks
50.0mg USD 250.0 2 Weeks
100.0mg USD 450.0 2 Weeks
200.0mg USD 850.0 2 Weeks
500.0mg USD 1850.0 2 Weeks
1.0g USD 2950.0 2 Weeks
2.0g USD 4850.0 2 Weeks
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Synonym: GSK2578215A; GSK-2578215A; GSK 2578215A.

IUPAC/Chemical Name: 2-(benzyloxy)-5-(2-fluoropyridin-4-yl)-N-(pyridin-3-yl)benzamide

InChi Key: WCIGMFCFPXZRMQ-UHFFFAOYSA-N

InChi Code: 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)

SMILES Code: O=C(NC1=CC=CN=C1)C2=CC(C3=CC(F)=NC=C3)=CC=C2OCC4=CC=CC=C4

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 399.43 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.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Yan J, Almilaji A, Schmid E, Elvira B, Shimshek DR, van der Putten H, Wagner CA, Shumilina E, Lang F. Leucine-rich repeat kinase 2-sensitive Na+/Ca2+ exchanger activity in dendritic cells. FASEB J. 2015 May;29(5):1701-10. doi: 10.1096/fj.14-264028. Epub 2015 Jan 21. PubMed PMID: 25609428.

2: Saez-Atienzar S, Bonet-Ponce L, Blesa JR, Romero FJ, Murphy MP, Jordan J, Galindo MF. 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. 2014 Aug 14;5:e1368. doi: 10.1038/cddis.2014.320. PubMed PMID: 25118928.

3: Reith AD, Bamborough P, Jandu K, Andreotti D, Mensah L, Dossang P, Choi HG, Deng X, Zhang J, Alessi DR, Gray NS. 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. doi: 10.1016/j.bmcl.2012.06.104. Epub 2012 Jul 7. PubMed PMID: 22863203; PubMed Central PMCID: PMC4208292.

 



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