WP1130

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WP1130

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Cat No: 15227

Biochemicals - Small Molecule Inhibitors

Protein ubiquitination is a dynamic process that can be reversed by deubiquitinating enzymes (DUBs) that remove ubiquitin from proteins, sparing them from degradation by the proteasome. The DUBs have been divided into two subgroups: ubiquitin-specific ...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

(2E)-3-(6-bromo-2-pyridinyl)-2-cyano-N-[1S-phenylbutyl]-2-propenamide

Correlated keywords:

Bcr/Abl anticancers Bcr Abl degrasyn deubiquintinase inhibitors inhibits inhibitions anti-tumors anti tumors antitumor bortezomib therapy therapies ubiquitin specific ubiquitin-specific protease apoptosis MCL-1 p53 MCL1 MCl 1 one WPs WP-1130 1130 tyrphostin derivatives deubiquitinating tumors proteins ubiquitination enzymes DUBs degradation proteasomes USPs UCHs COOH-terminal COOH terminal hydrolases activated cells transformed phenotypes WP1130 second-generation second generations USP9x 9x 9 x USP5 5 USP14 14 UCH37 37 tumor-activated induces accumulations protein-ubiquitin conjugates formations aggresomes mechanisms downregulates downs regulates down-regulate antiapoptotic Jak2 Jak 2 upregulates up up-regulate proapoptotic pro p 53

Product Overview:
Protein ubiquitination is a dynamic process that can be reversed by deubiquitinating enzymes (DUBs) that remove ubiquitin from proteins, sparing them from degradation by the proteasome. The DUBs have been divided into two subgroups: ubiquitin-specific proteases (USPs) and ubiquitin-specific COOH-terminal hydrolases (UCHs). Recent evidence suggests that several DUBs are activated in tumor cells and many contribute to a transformed phenotype.{24477} WP1130 is a second-generation tyrphostin derivative that inhibits the deubiquitinase activity of USP9x, USP5, USP14, and UCH37.{24478,24477} At 5 μM, WP1130-mediated inhibition of tumor-activated DUBs induces a rapid accumulation of protein-ubiquitin conjugates, resulting in the formation of aggresomes and apoptosis in a variety of tumor cells.{24477} Through this mechanism, WP1130 has been shown to downregulate the antiapoptotic proteins Bcr/Abl and Jak2 and to upregulate the proapoptotic proteins MCL-1 and p53.{24477}

Size	5 mg
Shipping	dry ice
CAS Number	856243-80-6
Molecular Formula	C₁₉H₁₈BrN₃O
SMILES	BrC1=NC(/C=C(C(N[C@H](C2=CC=CC=C2)CCC)=O)\C#N)=CC=C1
Molecular Weight	384,3
Formulation	A crystalline solid
Purity	≥95%
Custom Code	2837.19
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.