P005091

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P005091

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Cat No: 15224

Biochemicals - Small Molecule Inhibitors

Ubiquitin-specific proteases (USP/UBP) remove ubiquitin from proteins, sparing them from degradation by the proteasome. USP7 is a cysteine protease associated with prostate cancer that selectively deubiquitylates HDM2, the ubiquitin E3 ligase for the t...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

1-[5-[(2,3-dichlorophenyl)thio]-4-nitro-2-thienyl]-ethanone

Correlated keywords:

ubiquitin-specific ubiquitins specifics proteases USPs UBPs ubiquitylation proteasome USP7 cysteines USP-7 7 seven prostate cancers deubiquitylation HDM2 HDMs HDM-2 2 two E3 ligase tumors suppressors p53 anticancer anti-cancer anti multiple myeloma bortezomib therapy therapies deubiquintinase DUB selective USP/UBP P-005091 Ps 005091 P-5091 P5091 5091 trisubtituted thiophene inhibits inhibitions inhibitors caspases cathepsins calpain metalloproteases serines myeloma doxorubicin etoposide mechlorethamine in vivos B B-cells Bcells leukemia growths intracellular signaling P5091 HCT-116

Product Overview:
Ubiquitin-specific proteases (USP/UBP) remove ubiquitin from proteins, sparing them from degradation by the proteasome. USP7 is a cysteine protease associated with prostate cancer that selectively deubiquitylates HDM2, the ubiquitin E3 ligase for the tumor suppressor p53. P005091 is a trisubstituted thiophene that inhibits USP7 and the closely related USP47 (EC50s = 4.2 and 4.3 μM, respectively) with little activity against other classes of proteases, including caspases, cathepsins, calpain, metalloproteases, and serine proteases (EC50s = > 100 μM).{24461,24462} P005091 has been shown to accelerate the degradation of the USP7 substrate HDM2 in several multiple myeloma cell lines (EC50 = 11 μM) and to inhibit the growth of HCT116 human colorectal cancer cells (EC50 = 11 μM) synergistically with doxorubicin, etoposide, or mechlorethamine.{24461} In vivo, 10 mg/kg P005091 prolongs survival and reduces tumor growth in mice bearing human multiple myeloma and B cell leukemia xenografts.{24461}

Size	5 mg
Shipping	dry ice
CAS Number	882257-11-6
Molecular Formula	C₁₂H₇Cl₂NO₃S₂
SMILES	ClC1=C(Cl)C(SC2=C([N+]([O-])=O)C=C(C(C)=O)S2)=CC=C1
Molecular Weight	348,2
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2903.99
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.