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SML1925 Sigma-Aldrich

Bepristat 2a hydrochloride

≥95% (HPLC)

Synonym: 6-Bromo-2-[[[2-(diethylamino)ethyl]amino]methyl]-5-hydroxy-1-phenyl-1H-indole-3-carboxylic acid ethyl ester hydrochloride

  • Empirical Formula (Hill Notation) C24H30BrN3O3 · xHCl

  • Molecular Weight 488.42 (free base basis)

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Properties

Related Categories Apoptosis and Cell Cycle, B, Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology,
Quality Level   100
assay   ≥95% (HPLC)
form   powder
color   white to beige
solubility   H2O: 10 mg/mL, clear
storage temp.   2-8°C
SMILES string   CCN(CC)CCNCC1=C(C(OCC)=O)C2=CC(O)=C(Br)C=C2N1C3=CC=CC=C3.[H]Cl

Description

Biochem/physiol Actions

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.

Safety & Documentation

Safety Information

RIDADR 
NONH for all modes of transport
WGK Germany 
WGK 3
Flash Point(F) 
Not applicable
Flash Point(C) 
Not applicable

Documents

Certificate of Analysis (COA)

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Protocols & Articles
Peer-Reviewed Papers
15

References

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