[CAS NO. 1285515-21-0] GSK2578215A

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PRODUCTS SPECIFICATIONS [1285515-21-0]

Catalog

SLK-S7664

Brand

Selleck

CAS

1285515-21-0

DESCRIPTION [1285515-21-0]

Overview

MDL	MFCD22665702
Molecular Weight	399.42
Molecular Formula	C24H18FN3O2
SMILES	O=C(NC1=CC=CN=C1)C2=CC(C3=CC(F)=NC=C3)=CC=C2OCC4=CC=CC=C4

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.5036 mL	12.5182 mL	25.0363 mL
5 mM	0.5007 mL	2.5036 mL	5.0073 mL
10 mM	0.2504 mL	1.2518 mL	2.5036 mL
50 mM	0.0501 mL	0.2504 mL	0.5007 mL

Description

GSK2578215A is a potent and selective inhibitor with of 8.9 nM and 10.9 nM for LRRK2 (G2019S) and LRRK2 (WT), respectively.

Targets

LRRK2 (G2019S) ^[1]	LRRK2 (WT) ^[1]
8.9 nM	10.9 nM

In vitro

GSK2578215A induces a dose-dependent inhibition of Ser910 and Ser935 phosphorylation in both wild-type LRRK2 and LRRK2[G2019S] stably transfected into HEK293 cells, and induces similar dose-dependent Ser910 and Ser935 dephosphorylation of endogenous LRRK2 in mouse Swiss 3T3 cells. In SH-SY5Y cells, GSK2578215A impairs the autophagy flux by altering autophagosome–lysosome fusion, and induces mitophagy though induction of Drp-1-mediated mitochondrial fission and mitochondrial-derived ROS signaling.

In vivo

In vivo, GSK2578215A (100 mg/kg i.p.) inhibits Ser910 and Ser935 phosphorylation in mouse spleen and kidney, but not in brain.

References

[1] Reith AD, et al. Bioorg Med Chem Lett. 2012, 22(17), 5625-5629.
[2] Saez-Atienzar S, et al. Cell Death Dis. 2014, 5, e1368.