A potent

MK-0752 – 5 mg

Brand:
Cayman
CAS:
471905-41-6
Storage:
-20
UN-No:
Non-Hazardous - /

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}  

 

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Description

A potent, reversible inhibitor of γ-secretase, reducing the cleavage of APP to Aβ40 in SH-SY5Y cells with an IC50 value of 5 nM; 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

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

Synonyms: 

Molecular weight: 442.9

CAS: 471905-41-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Research Area|Cancer|Cell Signaling|Notch Signaling||Research Area|Cell Biology|Cell Signaling|Notch Signaling||Research Area|Cell Biology|Proteolysis|Lysosomal Proteases||Research Area|Cell Biology|Stem Cell Research||Research Area|Neuroscience|Neurodegenerative Disorders|Alzheimer’s Disease

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