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Chemical Structure| 1285515-21-0 Chemical Structure| 1285515-21-0

Structure of GSK2578215A
CAS No.: 1285515-21-0

Chemical Structure| 1285515-21-0

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GSK2578215A is a brain-penetrant, potent and selective LRRK2 inhibitor with IC50 values of 8.9 and 10.1 nM for LRRK2[G2019S] mutant and wild-type LRRK2, respectively.

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Product Details of GSK2578215A

CAS No. :1285515-21-0
Formula : C24H18FN3O2
M.W : 399.42
SMILES Code : O=C(NC1=CC=CN=C1)C2=CC(C3=CC(F)=NC=C3)=CC=C2OCC4=CC=CC=C4
MDL No. :MFCD22665702
InChI Key :WCIGMFCFPXZRMQ-UHFFFAOYSA-N
Pubchem ID :68107965

Safety of GSK2578215A

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • LRRK2

    LRRK2 (WT), IC50:10.9 nM

    LRRK2 (G2019S), IC50:8.9 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
OVCAR8 cells 1 μM 24 hours Inhibited homologous recombination efficiency Clin Transl Med. 2021 Mar;11(3):e341
human CD14+ monocytes 1 μM 4 hours GSK2578215A enhances IFN-γ-induced LRRK2 and inflammatory molecule gene expression J Neuroimmune Pharmacol. 2020 Dec;15(4):794-800
Dendritic cells (DCs) 1 μM 24 hours To investigate the effect of GSK2578215A on Na+/K+ ATPase activity, results showed that GSK2578215A significantly decreased Na+/K+ ATPase activity. Sci Rep. 2017 Jan 25;7:41117
BV2 microglial cells 1 μM 1 hour GSK2578215A attenuated Mn-induced TNF-α mRNA levels and secretion Neurotoxicology. 2024 Jul;103:105-114
BV2 microglial cells 1 μM 1 hour GSK2578215A attenuated Mn-induced oxidative stress and cytotoxicity Neurotoxicology. 2024 Jul;103:105-114

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice OVCAR8 xenograft model Intraperitoneal injection 5 mg/kg Three times a week for 3 weeks Combination treatment with GSK2578215A and Olaparib significantly inhibited tumor growth Clin Transl Med. 2021 Mar;11(3):e341
Mice WT mice and LRRK2 transgenic mice Brain slice perfusion 1 μM and 3 μM 2-hour incubation or 30-minute perfusion To evaluate the effects of GSK2578215A on dopamine release and recovery, results showed no significant effects at concentrations of 1 μM and 3 μM. CNS Neurosci Ther. 2017 Feb;23(2):162-173

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.50mL

0.50mL

0.25mL

12.52mL

2.50mL

1.25mL

25.04mL

5.01mL

2.50mL

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