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方案
≥98% (HPLC)
表单
powder
颜色
white to light brown
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
ClC1=C(O)C=CC(CN2CCC(C(N(CC)C)=O)(CCOC3=CC=CC=C3)CC2)=C1
InChI key
AYJKPBTXOIHUFT-UHFFFAOYSA-N
生化/生理作用
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)
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
Roelof H Bekendam et al.
Nature communications, 7, 12579-12579 (2016-08-31)
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
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