PDI-IN-4
PDI-IN-4 is a highly selective inhibitor of human PDI (IC50=0.48 μM) with no significant cytotoxicity. PDI-IN-4 binds to PDI in a reversible manner, not only forming a covalent bond with the Cys400 residue but also engaging in hydrophobic interactions with other residues. By inhibiting the activation of GPIIb/IIIa, PDI-IN-4 effectively blocks platelet aggregation and thrombus formation. PDI-IN-4 can serve as an important tool reagent for thrombosis-related research.
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- Formule: C17H12F3NO2
- Masse moléculaire:319.28
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
PDI-IN-4 (compound 14d) (0.48-7.10 μM; 1 h) potently inhibits recombinant human PDI with an IC50 of 0.48 μM, and shows selective inhibition over PDIA3 and PDIA6 isoforms[1].
PDI-IN-4 (40 μM; 1 h) exhibits a reversible covalent binding mode with recombinant human PDI[1].
PDI-IN-4 (2-50 μM; 3 min) dose-dependently inhibits U46619-, collagen-, and thrombin-induced aggregation of washed human platelets with IC50 values of 3.5 μM, 13.0 μM, and 25.5 μM, respectively[1].
PDI-IN-4 (5 μM; 3 min) abolishes U46619-induced GPIIb/IIIa activation and reduces P-selectin expression by 52% in washed human platelets[1].
PDI-IN-4 (5 μM; 10 min) reduces thrombus formation by 36% in human whole blood perfused through collagen-coated flow chambers at an arterial shear rate of 1500 s−1[1].
PDI-IN-4 (5-40 μM; 24 h) shows no significant cytotoxicity toward HUVECs, A549, MDA-MB-231, or HepG2 cells at concentrations between 5 and 40 μM after 24 h of incubation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human umbilical vein endothelial cells/HUVECs, human lung cancer A549 cells, human breast cancer MDA-MB-231 cells, human liver cancer HepG2 cells
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Concentration:5-40 μM
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Incubation Time:24 h
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Result:Exhibited no significant cytotoxicity toward HUVECs, A549, MDA-MB-231, or HepG2 cells after 24 h of treatment.
Chemical Information
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Masse moléculaire 319.28
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Formule C17H12F3NO2
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SMILES
O=C(C1=CC=C(NC(C(C(F)(F)F)=C)=O)C=C1)C2=CC=CC=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)