A potent LRRK2 inhibitor (IC50 = 18.7 nM); selective for LRRK2 over 178 kinases

GNE-9605 – 5 mg

Brand:
Cayman
CAS:
1536200-31-3
Storage:
-20
UN-No:
De Minimis - 3077 / 9

GNE-9065 is an orally bioavailable and potent inhibitor of leucine-rich repeat kinase 2 (LRRK2; IC50 = 18.7 nM).{27842} It is selective for LRRK2 over 178 kinases, inhibiting only TAK1-TAB1 >50% at a concentration of 0.1 μM. GNE-9065 (10 and 50 mg/kg) inhibits LRRK2 Ser1292 autophosphorylation in BAC transgenic mice expressing human LRRK2 protein with the G2019S mutation found in families with autosomal Parkinson’s disease.  

 

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Description

A potent LRRK2 inhibitor (IC50 = 18.7 nM); selective for LRRK2 over 178 kinases, inhibiting only TAK1-TAB1 >50% at a concentration of 0.1 μM; inhibits LRRK2 Ser1292 autophosphorylation in BAC transgenic mice expressing human LRRK2 protein with the G2019S mutation

Formal name: rel-N2-[5-chloro-1-[(3R,4R)-3-fluoro-1-(3-oxetanyl)-4-piperidinyl]-1H-pyrazol-4-yl]-N4-methyl-5-(trifluoromethyl)-2,4-pyrimidinediamine

Synonyms: 

Molecular weight: 449.8

CAS: 1536200-31-3

Purity: ≥98%

Formulation: A crystalline solid

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

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