PAI-1 (Plasminogen activator inhibitor-1, also known as SERPINE1) is a member of serine protease inhibitor (SERPIN) family that acts as the primary inhibitor of two main mammalian plasminogen activators, urinary-type (uPA) and tissue-type (tPA).The physiological balance between thrombosis and fibrinolysis is regulated by PAI-1, the primary negative regulator of plasminogen activation. The labile compound PAI-1 can take on four different states: active, latent, cleaved, and target-bound.
Many cardiovascular diseases are correlated with high PAI-1 levels. In addition, PAI-1 is crucial for cell adhesion, senescence, cancer invasion, and tissue remodeling. Furthermore, the biological prognostic factor for breast cancer and a marker of a poor prognosis in other cancers, the PAI-1 level, have both received extensive validation. One of the plasma biomarkers linked to non-alcoholic fatty liver disease is PAI-1. Because of these associations, PAI-1 is a desirable pharmaceutical target.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V73280 | 28-O-β-D-Glucopyranosyl pomolic acid | 83725-24-0 | 28-O-β-D-Glucopyranosyl pomolic acid is a urokinase plasminogen activator (uPA) inhibitor (antagonist) with IC50 of 37.82 μM. |
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V6438 | Anecortave Acetate | 7753-60-8 | Anecortave acetate is a potent ocular vascular inhibitor. |
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V73279 | Glutaryl-Gly-Arg-AMC | 65147-16-2 | Glutaryl-Gly-Arg-AMC is a bioactive peptide substrate of urokinase plasminogen activator (uPA). |
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V1883 | Tiplaxtinin (PAI-039) | 393105-53-8 | Tiplaxtinin(PAI-039) is an orally bioactive and selective plasminogen activator inhibitor-1 (PAI-1) inhibitor with IC50 of 2.7 μM. |
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V3510 | TM 5275 sodium | 1103926-82-4 | TM5275 sodium is a novelorally active and potent small molecule inhibitor of plasminogen activator inhibitor-1 (PAI-1) whichinhibits various tumor cell lines with anIC50of 6.95 μM. |
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V2887 | TM-5441 | 1190221-43-2 | TM-5441 (EBP 883 and BMS-790052) is a novelorally active and potent small molecule inhibitor of plasminogen activator inhibitor-1 (PAI-1) whichinhibits various tumor cell lines withIC50values in the range of 9.7 and 60.3 μM. |
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V3165 | UK-371804 | 256477-09-5 | UK-371804 is a potent and selective inhibitor of urokinase-type plasmogen activator (uPA) with excellent potency (Ki=10 nM in an enzyme assay) and selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin). |
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