A selective

GNE-0877 – 1 mg

Brand:
Cayman
CAS:
1374828-69-9
Storage:
-20
UN-No:
Excepted Quantity - 3077 / 9

Leucine-rich repeat kinase 2 (LRRK2) is an enzyme that interacts with parkin, a ligase that is part of the ubiquitin-proteasome system that mediates the targeting of proteins for degradation. Loss of function of the parkin protein leads to dopaminergic cell death. The development of Parkinson’s disease has been strongly associated with mutations in the LRRK2 gene that lead to increased kinase activity. GNE 0877 is a selective, brain-penetrable LRRK2 inhibitor (Ki = 0.7 nM).{27842} It inhibits LRRK2 Ser1292 autophosphorylation in BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation with an IC50 value of 3 nM in vivo.{27842}  

 

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Description

A selective, brain-penetrable LRRK2 inhibitor (Ki = 0.7 nM); inhibits LRRK2 Ser1292 autophosphorylation in BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation (IC50 = 3 nM in vivo)

Formal name: α,α,3-trimethyl-4-[[4-(methylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-1H-pyrazole-1-acetonitrile

Synonyms: 

Molecular weight: 339.3

CAS: 1374828-69-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Neuroscience|Neurodegenerative Disorders|Parkinson’s Disease

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