2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. PAI-1

PAI-1

Plasminogen activator inhibitor-1

PAI-1

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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). As the main negative regulator of plasminogen activation, PAI-1 is an essential factor in regulation of the physiological balance between thrombosis and fibrinolysis. PAI-1 is a labile molecule that exists in four different forms: active, latent, cleaved and target bound form.

High PAI-1 levels are associated with many cardiovascular diseases. PAI-1 also plays important roles in cell migration, adhesion, senescence, cancer invasion and tissue remodeling. Moreover, the PAI-1 level was extensively validated as the biological prognostic factor in breast cancer and as a marker of a poor prognosis in other cancers. PAI-1 is also one of the plasma biomarkers associated with nonalcoholic fatty liver disease. These associations have made PAI-1 an attractive pharmaceutical target.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-122714
    SK-216
    		Inhibitor
    SK-216 is a plasminogen activator inhibitor-1 (PAI-1) inhibitor that acts as an anti-metastatic agent for human osteosarcoma and inhibits lung metastasis of human osteosarcoma.
    SK-216
  • HY-126361
    ZK824190
    ZK824190 is an orally available and selective urokinase plasminogen activator (uPA) inhibitor as a potential treatment for multiple sclerosis. IC50s of 237, 1600 and 1850 nM for uPA, tPA, and Plasmin, respectively.
    ZK824190
  • HY-117724
    AZ3976
    		Inhibitor 98.03%
    AZ3976 is a potent plasminogen activator inhibitor type 1 (PAI-1) inhibitor with an IC50 value of 26 μM in an enzymatic chromogenic assay. AZ3976 is active with an IC50 of 16 μM in a plasma clot lysis assay. AZ3976 does not bind to active PAI-1 but bound reversibly to latent PAI-1. AZ3976 inhibits PAI-1 by enhancing the latency transition of active PAI-1. AZ3976 displays profibrinolytic activities in a human plasma clot lysis assay.
    AZ3976
  • HY-117359
    UCD38B hydrochloride
    		Inhibitor 99.31%
    UCD38B hydrochloride is a cell permeant, competitive enzymatic uPA inhibitor with an IC50 value of 7 μM. UCD38B hydrochloride targets intracellular uPA causing mistrafficking of uPA into perinuclear mitochondria, reducing the mitochondrial membrane potential, and followed by the release of apoptotic inducible factor (AIF). UCD38B hydrochloride induces apoptosis.
    UCD38B hydrochloride
  • HY-101761A
    TM5441 sodium
    		Inhibitor
    TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), has IC50 values between 13.9 and 51.1 μM. TM5441 induces intrinsic apoptosis in several human cancer cell lines. TM5441 attenuates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence.
    TM5441 sodium
  • HY-N10227
    Geodin
    		Inhibitor
    Geodin, a fungal metabolite, shows antibacterial activity. Geodin also is an inhibitor of plasminogen activator inhibitor- 1 (PAI-1).
    Geodin
  • HY-137495
    GGACK
    		Inhibitor
    GGACK (H-Glu-Gly-Arg-CMK) is an irreversible substrate-like serine protease urokinase-type plasminogen activator (uPA) inhibitor.
    GGACK
  • HY-114330
    ZK824859
    		Inhibitor
    ZK824859 is an oral available and selective urokinase plasminogen activator (uPA) inhibitor with IC50s of 79 nM, 1580 nM and 1330 nM for human uPA, tPA, and plasmin, respectively.
    ZK824859
  • HY-N1533
    28-O-β-D-Glucopyranosyl pomolic acid
    28-O-β-D-Glucopyranosyl pomolic acid is a urokinase plasminogen activator inhibitor with IC50 at 37.82 μM.
    28-O-β-D-Glucopyranosyl pomolic acid
  • HY-122542
    PPACK
    		Inhibitor
    PPACK is a plasminogen activator (rt-PA) inhibitor. PPACK can inhibit changes in fibrin degradation products, plasminogen and alpha 2-antiplasmin. PPACK also inhibits the binding of rt-PA to plasma protease inhibitors.
    PPACK
  • HY-106508
    Fendosal
    		Inhibitor
    Fendosal (HP 129) is an orally active, potent non-steroidal anti-inflammatory agent. Fendosal (HP 129) is also an inhibitor of Plasminogen activator inhibitor-1 (PAI-1) .
    Fendosal
  • HY-P4338
    Glutaryl-Gly-Arg-AMC
    Glutaryl-Gly-Arg-AMC is a peptide substrate of urokinase plasminogen activator (uPA).
    Glutaryl-Gly-Arg-AMC
  • HY-101214A
    UK-371804 hydrochloride
    UK-371804 hydrochloride (compound 24) is a urokinase-type plasminogen activator (uPA) inhibitor with a Ki of 10 nM.
    UK-371804 hydrochloride
  • HY-123191
    CJ-463
    		Inhibitor
    CJ-463 is a potent and selective uPA inhibitor. CJ-463 has antitumor activity.
    CJ-463
  • HY-119160
    TM5007
    		Inhibitor
    TM5007 is a poent and orally active inhibitor of plasminogen activator inhibitor-1 (PAI-1) with an IC50 of 29 μM. TM5007 enhance fibrinolysis activity and inhibits coagulation. TM5007 also prevents the fibrotic process initiated by bleomycin in mouse lung.
    TM5007
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity