A selective and highly potent inhibitor of DLK; also inhibits phosphorylated JNK (IC50 = 30 nM); selective over other MAP kinases

GNE-3511 – 5 mg

Brand:
Cayman
CAS:
1496581-76-0
Storage:
-20
UN-No:
Non-Hazardous - /

GNE-3511 is a selective and highly potent inhibitor of dual leucine zipper kinase (DLK), also known as MAP3K12 (Ki = 500 pM).{34676} It also inhibits phosphorylated JNK (IC50 = 30 nM) and is highly selective for DLK over other MAP kinases (IC50 > 5,000 nM for MKK4 and MKK7), JNKs (IC50s = 129, 514, and 364 nM for JNK1, JNK2, and JNK3, respectively), and mixed-lineage kinases (MLKs; IC50s = 68, 767, and 602 nM for MLK1, MLK2, and MLK3, respectively). GNE-3511 protects primary neurons in an in vitro axon degeneration assay (IC50 = 107 nM). In an MPTP mouse model of Parkinson’s disease, a high dose of GNE-3511 (75 mg/kg) completely suppresses phosphorylated c-Jun (p-c-Jun) expression, while a low dose (37.5 mg/kg) moderately reduces its expression.  

 

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Description

A selective and highly potent inhibitor of DLK; also inhibits phosphorylated JNK (IC50 = 30 nM); selective over other MAP kinases, JNKs, and MLKs; protects primary neurons in an in vitro axon degeneration assay (IC50 = 107 nM); decreases p-c-Jun expression in a mouse MPTP model of Parkinson’s disease,

Formal name: 2-[[6-(3,3-difluoro-1-pyrrolidinyl)-4-[1-(3-oxetanyl)-4-piperidinyl]-2-pyridinyl]amino]-4-pyridinecarbonitrile

Synonyms: 

Molecular weight: 440.5

CAS: 1496581-76-0

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||Research Area|Neuroscience|Neuroprotection

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