A specific inhibitor of the proteolytic activity of Omi/HtrA2 (IC50 = 9.5 μM) that is naturally fluorescent

UCF 101 – 1 mg

Brand:
Cayman
CAS:
313649-08-0
Storage:
-20
UN-No:
Non-Hazardous - /

Mammalian Omi/HtrA2 is a serine protease localized in mitochondria with close homology to bacterial HtrA chaperones. It is released from the mitochondria in response to apoptotic stimuli whereupon it induces cell death through both a caspase-dependent manner and a mechanism that involves its protease activity. UCF 101 is an inhibitor of the proteolytic activity of Omi/HtrA2 (IC50 = 9.5 μM).{25354} It is highly specific for Omi/HtrA2, demonstrating less potent activity when tested against a panel of various other serine proteases (IC50s range from 200 to >500 μM).{25354} Additionally, UCF 101 is naturally fluorescent, thus enabling the visualization of its entry into cells.{25354} UCF 101 has been used to decrease cerebral infarct size in a rat model of cerebral ischemia, demonstrating neuroprotective effects by reducing apoptosis of cortical cells.{25355} It has also been reported to be protective of cardiomyocytes against ischemic injury through a mechanism that prevents Omi/HtrA2 proteolysis of Thanatos-associated protein 5, a cardiac-specific nuclear protein that controls cell cycle progression.{25356}  

 

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Description

A specific inhibitor of the proteolytic activity of Omi/HtrA2 (IC50 = 9.5 μM) that is naturally fluorescent, thus enabling the visualization of its entry into cells; has been reported to decrease cerebral infarct size in a rat model of cerebral ischemia and to be protective of cardiomyocytes against ischemic injury

Formal name: dihydro-5-[[5-(2-nitrophenyl)-2-furanyl]methylene]-1,3-diphenyl-2-thioxo-4,6(1H,5H)-pyrimidinedione

Synonyms: 

Molecular weight: 495.5

CAS: 313649-08-0

Purity: ≥98%

Formulation: A crystalline solid

Application|Fluorescence||Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Research Area|Cardiovascular System|Cardiovascular Diseases|Stroke||Research Area|Cardiovascular System|Heart||Research Area|Cell Biology|Cell Cycle||Research Area|Cell Biology|Cell Death|Apoptosis||Research Area|Cell Biology|Proteolysis

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