plasminogen activator inhibitor-1

Upamostat is an inhibitor of a serine protease and is a urokinase plasminogen activator (uPA) inhibitor.

ZK824190 is an orally available and selective inhibitor of urokinase plasminogen activator (uPA), with IC50 values of 237 nM for uPA, 1600 nM for tPA, and 1850 nM for Plasmin.

Tiplaxtinin (Tiplasinin)(PAI-039) is a selective and orally efficacious inhibitor of plasminogen activator inhibitor-1 (PAI-1) with IC50 of 2.7 uM.

Aleplasinin (PAZ 417) is a selective and orally active inhibitor of Plasminogen activator inhibitor-1(PAI-1) and a key negative regulator of the fibrinolytic system. Aleplasinin can be used in Alzheimer's disease studies.

UK-371804 is an effective and specific uPA inhibitor. It was selected as a candidate for further preClinicalal evaluation for the treatment of chronic dermal ulcers.

Loureirin B can downregulate the expression of fibrosis-related molecules by regulating MMPs and TIMPs levels, inhibit scar fibroblast proliferation and suppress TGF-β1-induced fibrosis, during which TGF-β1/Smad2/3 pathway is likely involved.

TM5441 is an orally bioavailable fibrinogen activator inhibitor-1 inhibitor that inhibits several cancer cell lines with IC50 values ranging from 13.9 to 51.1 μM.It induces intrinsic cell death in several human cancer cells and attenuates Nω-nitro-1-arginine methyl ester-induced cardiac hypertension and vascular senescence.

TM5275 sodium is a bioactive oral inhibitor of PAI-1 (plasminogen activator inhibitor-1), with an IC50 value of 6.95 μM.

Toddalolactone ((+)-Toddalolactone) is an anti-inflammatory and analgesic.

TM5007 is a poent inhibitor of plasminogen activator inhibitor-1 (PAI-1; IC50 of 29 uM).

SK-216, a specific PAI-1 inhibitor, reduces tumor angiogenesis and inhibits VEGF-induced migration and tube formation of human umbilical vein endothelial cells in vitro. This compound also alleviates bleomycin-induced pulmonary fibrosis in mice.

4-Aminobenzamidine dihydrochloride (p-Aminobenzamidine dihydrochloride) is a strong trypsin inhibitor and a relatively weak inhibitor of urokinase type plasminogen activator (uPA) (K i =82 μM). 4-Aminobenzamidine can inhibit growth of a human prostate tumor in SCID mice [1] [2].

UKI-1 is a urokinase-type plasminogen activator system synthetic inhibitor.

CDE-096 is a potent inhibitor of plasminogen activator inhibitor-1 that prevents PAI-1–mediated inactivation of tissue plasminogen activator and urokinase plasminogen activator with nanomolar potency, while maintaining activity against glycosylated and multispecies PAI-1, enabling translational research in fibrinolysis and thrombosis regulation.

Diaplasinin (PAI-749) is a highly efficient inhibitor of plasminogen activator inhibitor-1 (PAI-1) with antithrombotic activity. It can be used in cardiovascular disease research.

GGACK is an inhibitor of urokinase-type plasminogen activator (uPA) and factor Xa (Kis = 1.8 and 8.7 μM, respectively).1,2 1.Kettner, C., and Shaw, E.The susceptibility of urokinase to affinity labeling by peptides of arginine chloromethyl ketoneBiochim. Biophys. Acta569(1)31-40(1979) 2.Kettner, C., and Shaw, E.The selective affinity labeling of factor Xa by peptides of arginine chloromethyl ketoneThromb. Res.22(5-6)645-652(1981)

IMD-1622 is a plasminogen activator inhibitor-1 (PAI-1) inhibitor.

XR 1853 is a low molecular weight modulator of human plasminogen activator inhibitor-1 activity.

THR-18 is an 18-mer peptide derived from the sequence of human plasminogen activator inhibitor 1 (PAI-1), having the ability to bind to a site of tissue plasminogen activator (tPA) distal to its catalytic site and uncouple the beneficial clot-dissolving properties of tPA from its deleterious non-fibrinolytic effects.

TM5441, an orally bioavailable plasminogen activator inhibitor-1 (PAI-1) inhibitor with IC50 values ranging from 13.9 to 51.1 μM, effectively induces intrinsic apoptosis across multiple human cancer cell lines. Additionally, it mitigates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence [1] [2].

Anti-SERPINE1 Antibody is a humanized monoclonal antibody targeting Serpin Family E Member 1 (SERPINE1/PAI-1). SERPINE1, also known as Plasminogen Activator Inhibitor-1 (PAI-1), is the primary physiological inhibitor of tissue-type (tPA) and urokinase-type (uPA) plasminogen activators, playing a critical role in regulating fibrinolysis, cell migration, and tissue remodeling. Elevated PAI-1 levels are associated with thrombosis, fibrosis, metabolic syndrome, and tumor progression (including immune evasion and metastasis). Anti-SERPINE1 Antibody specifically binds to PAI-1, neutralizing its inhibitory activity and restoring tPA/uPA-mediated plasmin generation to promote fibrinolysis and reduce extracellular matrix deposition. Additionally, the antibody blocks PAI-1-mediated upregulation of PD-L1, thereby enhancing anti-tumor immune responses in the tumor microenvironment, and possesses potential anti-senescence properties.

PAI-1 is a plasminogen activator inhibitor. It belongs to the serine protease (Ser Protease) inhibitor superfamily and exhibits antiprotease activity. PAI-1 is the primary physiological inhibitor of tissue-type (tPA) and urokinase-type (uPA) plasminogen activators (PAs).