Bepristat 1a is a selective reversible inhibitor of protein disulfide isomerase (PDI), an enzyme in the endoplasmic reticulum that catalyzes disulfide bond breakage and reformation to catalyze protein folding. Unlike most PDI inhibitors, Bepristat 1a binds at the substrate-binding site, rather than the catalytic site. It blocked PDI activity with an IC50 value of 700 nM. PDI is up-regulated in several cancers, has been implicated in neurodegenerative processes, and plays an important role in thrombus formation. Bepristat 1a potently inhibited platelet aggregation and thrombus formation in vivo.
Selective reversible inhibitor of protein disulfide isomerase (PDI)
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Protein disulfide isomerase (PDI) is an oxidoreductase essential for folding proteins in the endoplasmic reticulum. The domain structure of PDI is a-b-b'-x-a', wherein the thioredoxin-like a and a' domains mediate disulfide bond shuffling and b and b' domains are substrate
Numer pozycji handlu globalnego
SKU
NUMER GTIN
SML2164-25MG
04061835502950
SML2164-5MG
04061835502967
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