MK-0752

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MK-0752

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Cat No: 16706

Biochemicals - Small Molecule Inhibitors

γ-Secretase is a protease complex that cleaves single-pass transmembrane proteins, such as Notch receptors and β-amyloid precursor protein (APP), within the transmembrane domain.{27051,25415} MK-0752 is a potent, reversible inhibitor of γ-secretase, re...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)-cyclohexanepropanoic acid

Correlated keywords:

952578-?68-?6 656810-87-6 biochemical inhibitor inhibit Alzheimer’s research neuroscience cancer stem cell research MK0752 potent ?-secretase protease complex cleave single-pass transmembrane protein Notch receptor precursor ?-amyloid APP domain reversible A?40 A?-40 cleavage reduce human neuroblastoma SH-SY5Y SHSY5Y orally bioavailable blood-brain barrier dose-dependently generation new rhesus monkey pathway breast cancer tumorgraft chemotherapy drug docetaxel mice tumor

Product Overview:
γ-Secretase is a protease complex that cleaves single-pass transmembrane proteins, such as Notch receptors and β-amyloid precursor protein (APP), within the transmembrane domain.{27051,25415} MK-0752 is a potent, reversible inhibitor of γ-secretase, reducing the cleavage of APP to Aβ40 in human neuroblastoma SH-SY5Y cells with an IC50 value of 5 nM.{27408,27409} It is orally bioavailable and crosses the blood-brain barrier, as orally administered MK-0752 dose-dependently reduces the generation of new amyloid β protein in the brain of rhesus monkeys.{27409} Through its effects on the Notch pathway, MK-0752 reduces the number of breast cancer stem cells in tumorgrafts, enhancing the efficacy of the chemotherapy drug docetaxel (Item No. 11637) in mice with breast cancer tumors.{27410}

Size	1 mg
Shipping	dry ice
CAS Number	471905-41-6
Molecular Formula	C₂₁H₂₁ClF₂O₄S
SMILES	O=C(O)CC[C@H]1CC[C@](S(C2=CC=C(Cl)C=C2)(=O)=O)(C3=C(F)C=CC(F)=C3)CC1
Molecular Weight	442,9
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.

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.