GNE-0877

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GNE-0877

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Cat No: 16251

Biochemicals - Kinase Inhibitors

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...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

?,?,3-trimethyl-4-[[4-(methylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-1H-pyrazole-1-acetonitrile

Correlated keywords:

neuroscience Leucine-rich repeat kinase 2 LRRK2 inhibitor Parkinson’s disease mutation biochemical inhibit selective GNE0877 brain-penetrable Ser1292 Ser 1292 autophosphorylation protein G2019S in vivo

Product Overview:
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}

Size	500 µg
Shipping	dry ice
CAS Number	1374828-69-9
Molecular Formula	C₁₄H₁₆F₃N₇
SMILES	CNC1=C(C(F)(F)F)C=NC(NC2=CN(C(C)(C#N)C)N=C2C)=N1
Molecular Weight	339,3
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2933.19
UNSPSC code	12352100

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.