Territorial Availability: Available through Bertin Technologies only in France
- Synonyms
- 1-[5-[(2,4-difluorophenyl)thio]-4-nitro-2-thienyl]-ethanone
- Correlated keywords
- P-22077 USP-7 47 HEK-293 HDM-2 p-53
- Product Overview:
P22077 is a dual inhibitor of the deubiquitylating enzymes ubiquitin-specific protease 7 (USP7) and USP47 (EC50s = 8.01 and 8.74 µM, respectively, in a fluorescence-based enzyme assay).{27951} It is selective for USP7 and USP47 over other USPs and proteases with EC50 values greater than 50 µM. P22077 (25 µM) induces the accumulation of polyubiquitinated proteins in HEK293 cells. In neuroblastoma cells in vitro, P22077 blocks deubiquitylation of HDM2, a protein that normally deubiquitinates the tumor suppressor p53 leading to its degradation.{39388} When used at concentrations of 10 and 20 µM, it amplifies the cytotoxicity and p53-mediated apoptosis of doxorubicin (Item No. 15007) and etoposide (Item No. 12092) in neuroblastoma cells. P22077 inhibits tumor growth in neuroblastoma mouse xenograft models when administered at a dose of 20 mg/kg per day.
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.