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GSK 2578215A
Axon 2181
CAS:
1285515-21-0
Purity:
99%
- Soluble in DMSO
- MF: C24H18FN3O2
- MW: 399.42
Description
GSK 2578215A is a potent and highly selective LRRK2 inhibitor with reported IC50 values of 10.9 nM for wild-type LRRK2 and 8.9 nM for the LRRK2 G2019S mutant. It has reported blood-brain barrier permeability and favorable brain-to-plasma distribution in mice.
LRRK2 mutations are linked to familial and sporadic Parkinson disease, and LRRK2 kinase activity regulates vesicular trafficking, inflammation and neuronal stress pathways. GSK 2578215A is relevant for LRRK2 target-validation studies.
Key Features
- Potent LRRK2 kinase inhibitor
- Active against wild-type and G2019S mutant LRRK2
- Highly selective kinase profile reported
- Brain exposure reported in mouse studies
Applications
- LRRK2 (Leucine-rich repeat kinase 2) kinase assays
- Parkinson disease model research
- Neurodegeneration pathway studies
- Brain-penetrant kinase inhibitor profiling
More Information
| Parent CAS No. | 1285515-21-0 |
|---|---|
| Chemical Name | 2-(benzyloxy)-5-(2-fluoropyridin-4-yl)-N-(pyridin-3-yl)benzamide |
| SMILES | C(NC1=CC=CN=C1)(=O)C1=CC(C2C=CN=C(F)C=2)=CC=C1OCC1=CC=CC=C1 |
| MFCD | N.A. |
| InChi | InChI=1S/C24H18FN3O2/c25-23-14-19(10-12-27-23)18-8-9-22(30-16-17-5-2-1-3-6-17)21(13-18)24(29)28-20-7-4-11-26-15-20/h1-15H,16H2,(H,28,29) |
| InChiKey | WCIGMFCFPXZRMQ-UHFFFAOYSA-N |
| CID | 68107965 |
| Short Description | LRRK2 inhibitor |
References
- A.D. Reith et al. GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor. Bioorg. Med. Chem. Lett. 2012, 22, 5625-5629.
- M.E. Kavanagh et al. The development of CNS-active LRRK2 inhibitors using property-directed optimisation. Bioorg. Med. Chem. Lett. 2013, 23, 3690-3696.
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