CAY10681

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CAY10681

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Cat No: 15573

Biochemicals - Small Molecule Inhibitors

Inactivation of the tumor suppressor p53 commonly coincides with increased signaling through NF-κB in cancer. CAY10681 is a dual modulator of p53-MDM2 interaction and NF-κB signaling.{25314} It potently binds MDM2 (Ki = 250 nM), reducing MDM2-mediated ...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

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

Correlated keywords:

biochemical inhibitor cancer intracellular signaling gene regulation inflammation NF-?B dual modulator p53-MDM2 interaction bind mediated turnover inhibit phosphorylation I?B? reduce reduction nuclear accumulation p65 block proliferation cell line oral bioavailability bioavailable tumor growth A549 xenograft in vivo vitro

Product Overview:
Inactivation of the tumor suppressor p53 commonly coincides with increased signaling through NF-κB in cancer. CAY10681 is a dual modulator of p53-MDM2 interaction and NF-κB signaling.{25314} It potently binds MDM2 (Ki = 250 nM), reducing MDM2-mediated turnover of p53.{25314} CAY10681 also inhibits phosphorylation of IκBα and dose-dependently reduces nuclear accumulation of p65.{25314} It blocks the proliferation of cancer cell lines (IC50s range from 33 to 37 µM).{25314} CAY10681 exhibits excellent oral bioavailability and inhibits tumor growth in A549 xenografts in nude mice.{25314}

Size	1 mg
Shipping	dry ice
CAS Number	1542066-69-2
Molecular Formula	C₃₀H₂₆BrN₅O
SMILES	O=C1N(CCCN2C=CN=C2)C(C3=CC=C(Br)C=C3)C4=C1N(CC5=CC=CC=C5)N=C4C6=CC=CC=C6
Molecular Weight	552,5
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2933.29
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.

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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.