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SML0660

Sigma-Aldrich

GSK2578215A

≥98% (HPLC)

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Synonym(s):
5-(2-Fluoro-4-pyridinyl)-2-(phenylmethoxy)-N-3-pyridinyl-benzamide
Empirical Formula (Hill Notation):
C24H18FN3O2
CAS Number:
Molecular Weight:
399.42
NACRES:
NA.77

Quality Level

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 15 mg/mL, clear

storage temp.

2-8°C

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)

InChI key

WCIGMFCFPXZRMQ-UHFFFAOYSA-N

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This Item
G7423SML2762SML0709
Sigma-Aldrich

SML0660

GSK2578215A

GSK3787 ≥98% (HPLC), white to off-white, powder

G7423

GSK3787

RG1534 ≥98% (HPLC)

SML2762

RG1534

GSK-J1 ≥98% (HPLC)

SML0709

GSK-J1

form

powder

form

powder

form

powder

form

powder

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

solubility

DMSO: 15 mg/mL, clear

solubility

DMSO: ≥10 mg/mL

solubility

DMSO: 2 mg/mL, clear

solubility

DMSO: 15 mg/mL, clear

color

white to beige

color

white to off-white

color

white to beige

color

white to beige

Biochem/physiol Actions

GSK2578215A is a potent inhibitor of leucine-rich repeat 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 that 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 Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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The LRRK2 inhibitor GSK2578215A induces protective autophagy in SH-SY5Y cells: involvement of Drp-1-mediated mitochondrial fission and mitochondrial-derived ROS signaling
Saez-Atienzar S, et al.
Cell Death & Disease, 5(8), e1368-e1368 (2014)

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