GSK2578215A

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.

Product Specifications

CAS Number

[1285515-21-0]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Autophagy; LRRK2; Mitophagy

Type

Reference compound

Related Pathways

Autophagy

Applications

Neuroscience-Neuromodulation

Field of Research

Cancer; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/GSK2578215A.html

Concentration

10mM

Purity

99.82

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

FC1=NC=CC(C2=CC(C(NC3=CC=CN=C3)=O)=C(OCC4=CC=CC=C4)C=C2)=C1

Molecular Formula

C24H18FN3O2

Molecular Weight

399.42

Precautions

H302, H315, H319, H335

References & Citations

[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.|[2]Saez-Atienzar S, et al. 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 (8) :e1368.|[3]Chen L, et al. LRRK2 inhibition potentiates PARP inhibitor cytotoxicity through inhibiting homologous recombination-mediated DNA double strand break repair. Clin Transl Med. 2021 Mar;11 (3) :e341.