GSK180736A

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GSK180736A

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Cat No: 26182

Biochemicals - Kinase Inhibitors

GSK180736A is an inhibitor of Rho-associated kinase 1 (ROCK1; IC50 = 14 nM) and G protein-coupled receptor kinase 2 (GRK2; IC50 = 0.77 µM).{26327,42595} It is selective for GRK2 over GRK1, GRK5, and PKA (IC50 = >100 µM for all) and selective for R...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

4-(4-fluorophenyl)-1,2,3,4-tetrahydro-N-1H-indazol-5-yl-6-methyl-2-oxo-5-pyrimidinecarboxamide

Correlated keywords:

GSK-180736A 180736-A GSK180736-A ROCKI GRK-1 2 5 RSK-1 p-20S6K 20S6-K GPCR

Product Overview:
GSK180736A is an inhibitor of Rho-associated kinase 1 (ROCK1; IC50 = 14 nM) and G protein-coupled receptor kinase 2 (GRK2; IC50 = 0.77 µM).{26327,42595} It is selective for GRK2 over GRK1, GRK5, and PKA (IC50 = >100 µM for all) and selective for ROCK1 over RSK1 and p20S6K (IC50s = 3,100 and 2,850 nM, respectively).{26327,42595} GSK180736A increases maximum contractility in isolated mouse cardiomyocytes when used at a concentration of 1 µM.{42595}

Size	5 mg
Shipping	dry ice
CAS Number	817194-38-0
Molecular Formula	C₁₉H₁₆FN₅O₂
SMILES	FC1=CC=C(C2NC(NC(C)=C2C(NC3=CC=C(NN=C4)C4=C3)=O)=O)C=C1
Molecular Weight	365,4
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2903.99
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.