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GSK2578215A LRRK2 inhibitor

Cat.No.S7664

GSK2578215A is a potent and selective LRRK2 kinase inhibitor with IC50 of 8.9 nM and 10.9 nM for LRRK2 (G2019S) and LRRK2 (WT), respectively.
GSK2578215A LRRK2 inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 399.42

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S766401 DMSO]79 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.88%
99.88

Chemical Information, Storage & Stability

Molecular Weight 399.42 Formula

C24H18FN3O2

 Storage (From the date of receipt)
CAS No. 1285515-21-0 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1=CC=C(C=C1)COC2=C(C=C(C=C2)C3=CC(=NC=C3)F)C(=O)NC4=CN=CC=C4

Solubility

In vitro
Batch:

DMSO : 79 mg/mL (197.78 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Mechanism of Action

Targets/IC50/Ki
LRRK2 (G2019S) [1]
8.9 nM
LRRK2 (WT) [1]
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. [1] In SH-SY5Y cells, this compound 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. [2]
In vivo
In vivo, GSK2578215A (100 mg/kg i.p.) inhibits Ser910 and Ser935 phosphorylation in mouse spleen and kidney, but not in brain. [1]
References

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