GSK256066

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GSK256066

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Cat No: 28012

Biochemicals - Small Molecule Inhibitors

GSK256066 is a potent phosphodiesterase 4 (PDE4) inhibitor (IC50s = 4.9, 3.2, 3.8, and 1.1 pM for PDE4A, PDE4B, PDE4C, and PDE4D, respectively).{47799} It is greater than 380,000-fold selective for PDE4 over PDE1-3, -5, and -6 and greater than 2,500-f...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

6-[[3-[(dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide

Correlated keywords:

GSK 256066 PDE 4 4A 4B 4C 4D PDE2 PDE3 PDE5 PDE6 TNF?

Product Overview:
GSK256066 is a potent phosphodiesterase 4 (PDE4) inhibitor (IC50s = 4.9, 3.2, 3.8, and 1.1 pM for PDE4A, PDE4B, PDE4C, and PDE4D, respectively).{47799} It is greater than 380,000-fold selective for PDE4 over PDE1-3, -5, and -6 and greater than 2,500-fold selective over PDE7. GSK256066 inhibits LPS-induced TNF-α production in human peripheral blood monocytes (IC50 = 0.01 nM) and human whole blood (IC50 = 126 pM). Intratracheal administration of GSK256066 inhibits LPS-induced pulmonary neutrophilia in rats (ED50 = 1.1 µg/kg). It inhibits ovalbumin-induced pulmonary eosinophilia in rats (ED50 = 0.4 µg/kg) and LPS-induced pulmonary neutrophilia in ferrets (ED50 = 18 µg/kg).{47800}

Size	1 mg
Shipping	dry ice
CAS Number	801312-28-7
Molecular Formula	C₂₇H₂₆N₄O₅S
SMILES	O=C(N(C)C)C1=CC=CC(S(C2=CC(C(NC3=CC=CC(OC)=C3)=C(C(N)=O)C=N4)=C4C(C)=C2)(=O)=O)=C1
Molecular Weight	518,6
Formulation	A solid
Purity	≥98%
Custom Code	2930.90
UNSPSC code	12352100

Technical File

MSDS

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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.