CAY10682

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CAY10682

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Cat No: 15574

Biochemicals - Small Molecule Inhibitors

(±)-Nutlin-3 (Item No. 10004372) blocks the interaction of p53 with its negative regulator Mdm2 (IC50 = 90 nM), inducing the expression of p53-regulated genes and blocking the growth of tumor xenografts in vivo.{11628} CAY10682 is a pyrrolo[3,4c]pyrazo...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

4-(4-bromophenyl)-1-[(4-fluorophenyl)methyl]-4,5-dihydro-5-[3-(1H-imidazol-1-yl)propyl]-3-phenyl-pyrrolo[3,4-c]pyrazol-6(1H)-one

Correlated keywords:

biochemicals cancer intracellular signaling dual interaction inhibitors inhibit gene regulation NF-?B NF?B pathyway p53-Mdm2 p53Mdm2 interaction pyrrolo[3,4c]pyrazole derivative (+)-nutlin-3 phosphorylation of I?B? kinase IKK? IKK? IKK? A549 cell xenograft CAY 10682

Product Overview:
(±)-Nutlin-3 (Item No. 10004372) blocks the interaction of p53 with its negative regulator Mdm2 (IC50 = 90 nM), inducing the expression of p53-regulated genes and blocking the growth of tumor xenografts in vivo.{11628} CAY10682 is a pyrrolo[3,4c]pyrazole derivative that inhibits the p53-Mdm2 interaction as potently as (±)-nutlin-3 (Ki = 83 nM) and also dose-dependently reduces activation of the NF-κB pathway.{25314} It specifically prevents phosphorylation of IκBα by the kinases IKKα, IKKβ, and IKKɛ (IC50s = 80.5, 78.2, and 57.1 µM, respectively).{25314} CAY10682 blocks the growth of cancer cells in vitro (IC50s = 2-6 µM) and inhibits the growth of A549 cell xenografts in mice without significantly reducing body weight.{25314}

Size	1 mg
Shipping	dry ice
CAS Number	1542066-74-9
Molecular Formula	C₃₀H₂₅BrFN₅O
SMILES	O=C1N(CCCN2C=CN=C2)C(C3=CC=C(Br)C=C3)C4=C1N(CC5=CC=C(F)C=C5)N=C4C6=CC=CC=C6
Molecular Weight	570,5
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.