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PAI-1

PAI-1

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.

PAI-1 related products

Structure Cat No. Product Name CAS No. Product Description
28-O-β-D-Glucopyranosyl pomolic acid 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.
Anecortave Acetate V6438 Anecortave Acetate 7753-60-8 Anecortave acetate is a potent ocular vascular inhibitor.
Glutaryl-Gly-Arg-AMC V73279 Glutaryl-Gly-Arg-AMC 65147-16-2 Glutaryl-Gly-Arg-AMC is a bioactive peptide substrate of urokinase plasminogen activator (uPA).
Tiplaxtinin (PAI-039) 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.
TM 5275 sodium 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.
TM-5441 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.
TM5441 sodium V84168 TM5441 sodium 2319722-53-5
UK-371804 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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