LRRK2-kinase inhibitor Chemical Properties

Boiling point:

556.1±50.0 °C(Predicted)

Density 

1.292±0.06 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

DMSO: soluble15mg/mL, clear

form 

powder

pka

12.31±0.70(Predicted)

color 

white to beige

Safety Information

WGK Germany 

3

LRRK2-kinase inhibitor Usage And Synthesis

Uses

GSK2578215A is a potent, selective LRRK2 inhibitor and a promising therapeutic for treating Parkinson''s disease.

Biological Activity

GSK2578215A is a potent inhibitor of leucine-rich repe at kinase-2 (LRRK2) also known as dardarin or PARK8, a kinase with mutations linked to Parkinson′s disease. Because the most common mutation, G2019S, enhances LRRK2 kinase activity, it is hoped th at LRRK2 inhibitors may be useful in treating the disease. GSK2578215A inhibited both wild-type and G2019S mutant LRRK2 kinase activity with IC50s of 10.9 and 8.9 nM respectively. It has good blood-brain barrier (BBB) permeability with a high ratio of brain to plasma distribution in mice.', 'GSK2578215A stimulates mitochondrial fragmentation, autophagy and mitophagy.

storage

Store at RT