所有图片(1)
别名:
6-Bromo-2-[[[2-(diethylamino)ethyl]amino]methyl]-5-hydroxy-1-phenyl-1H-indole-3-carboxylic acid ethyl ester hydrochloride
经验公式（希尔记法）:
C24H30BrN3O3 · xHCl
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质量水平
检测方案
≥95% (HPLC)
形式
powder
储存条件
desiccated
颜色
white to beige
溶解性
H2O: 10 mg/mL, clear
储存温度
2-8°C
SMILES字符串
CCN(CC)CCNCC1=C(C(OCC)=O)C2=CC(O)=C(Br)C=C2N1C3=CC=CC=C3.[H]Cl
生化/生理作用
Bepristat 2a 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 2a binds at the substrate-binding site, rather than the catalytic site. Bepristat 2a blocked PDI activity with an IC50 value of 1200 nM, while enhancing catalytic activity of remote PDI domains. PDI is up-regulated in several cancers, has been implicated in neurodegenerative processes, and plays an important role in thrombus formation. Bepristat 2a potently inhibited platelet aggregation and thrombus formation in vivo.
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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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