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-B0236A
    6-Aminocaproic acid hydrochloride
    		Inhibitor
    6-Aminocaproic acid hydrochloride, a monoamino carboxylic acid, is a potent and orally active inhibitor of plasmin and plasminogen. 6-Aminocaproic acid is a potent antifibrinolytic agent. 6-Aminocaproic acid prevents clot lysis through the competitive binding of lysine residues on plasminogen, inhibiting plasmin formation and reducing fibrinolysis. 6-Aminocaproic acid can be used for the research of bleeding disorders.
    6-Aminocaproic acid hydrochloride
  • HY-117537
    XR 5118 hydrochloride
    		Inhibitor
    XR 5118 hydrochloride is an inhibitor of plasminogen activator inhibitor 1 (PAI-1) (IC50: 12 µM). XR5118 binds to PAI-1 and reduces plasma PAI-1 activity levels. XR5118 hydrochloride promotes endogenous thrombolysis and inhibits thrombus accretion. XR 5118 hydrochloride can be used for research of cancer and thrombotic disease.
    XR 5118 hydrochloride
  • HY-132187S
    Sphingosylphosphorylcholine-d9
    		99.0%
    Sphingosylphosphorylcholine-d9 is deuterium labeled Sphingosylphosphorylcholine.
    Sphingosylphosphorylcholine-d<sub>9</sub>
  • HY-16512
    Upamostat hydrogen sulfate
    		Inhibitor
    Upamostat (WX-671) hydrogen sulfate, a prodrug of WX-UK1 (HY-100415), is an orally active serine protease inhibitor. Upamostat hydrogen sulfate inhibits the urokinase-type plasminogen activator (uPA) system, blocking the plasminogen activation process mediated by it, thereby suppressing the invasion, migration and metastasis of tumor cells. Upamostat hydrogen sulfate can be used in the research of metastatic breast cancer and locally advanced pancreatic cancer.
    Upamostat hydrogen sulfate
  • HY-B0236R
    6-Aminocaproic acid (Standard)
    		Inhibitor
    6-Aminocaproic acid (Standard) is the analytical standard of 6-Aminocaproic acid. This product is intended for research and analytical applications. 6-Aminocaproic acid (EACA), a monoamino carboxylic acid, is a potent and orally active inhibitor of plasmin and plasminogen. 6-Aminocaproic acid is a potent antifibrinolytic agent. 6-Aminocaproic acid prevents clot lysis through the competitive binding of lysine residues on plasminogen, inhibiting plasmin formation and reducing fibrinolysis. 6-Aminocaproic acid can be used for the research of bleeding disorders.
    6-Aminocaproic acid (Standard)
  • HY-P4341
    D-Val-Leu-Lys-AMC
    D-Val-Leu-Lys-AMC is a selective fluorogenic peptide substrate of plasmin. D-Val-Leu-Lys-AMC can be used for the quantification of enzymatic activity of plasmin. Ex: 360-380 nm, Em: 440-460 nm.
    D-Val-Leu-Lys-AMC
  • HY-100415S1
    UKI-1-d8 acetate
    		Inhibitor
    UKI-1-d8 acetate (WX-UK1-d8 acetate) is the deuterium labeled UKI-1 acetate. UKI-1 (WX-UK1) is a potent urokinase-type plasminogen activator (uPA) inhibitor with a Ki of 0.41 μM. UKI-1 is also a low molecular weight serine protease inhibitor. UKI-1 is a potent antimetastatic agent and inhibits the invasive capacity of carcinoma cells.
    UKI-1-d<sub>8</sub> acetate
  • HY-113769
    WB 3559 A
    		Activator
    WB 3559 A is a fibrinolytic plasminogen activator. WB 3559 A accelerates the conversion of plasminogen to plasmin and directly degrades fibrin in thrombi. WB 3559 A is promising for research of acute thrombotic diseases (e.g., myocardial infarction, pulmonary embolism).
    WB 3559 A
  • HY-N0518R
    Toddalolactone (Standard)
    		Inhibitor
    Toddalolactone (Standard) is the analytical standard of Toddalolactone. This product is intended for research and analytical applications. Toddalolactone, a main component of Toddalia asiatica, inhibits the activity of recombinant human plasminogen activator inhibitor-1 (PAI-1), with an IC50 value of 37.31 μM.
    Toddalolactone (Standard)
  • HY-P990504
    Anti-SERPINE1 Antibody
    		Inhibitor ≥99.0%
    Anti-SERPINE1 Antibody is a human-derived antibody expressed in CHO, targeting SERPINE1. The Anti-SERPINE1 Antibody has a huIgG1 type heavy chain and a huκ type light chain, with a predicted molecular weight (MW) of 150 kDa. The isotype control for Anti-SERPINE1 Antibody can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-SERPINE1 Antibody
  • HY-N1504R
    Loureirin B (Standard)
    		Inhibitor
    Loureirin B (Standard) is the analytical standard of Loureirin B. This product is intended for research and analytical applications. Loureirin B, a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of plasminogen activator inhibitor-1 (PAI-1), with an IC50 of 26.10 μM; Loureirin B also inhibits KATP, the phosphorylation of ERK and JNK, and has anti-diabetic activity.
    Loureirin B (Standard)
  • HY-114150B
    D-Val-Leu-Arg-pNA hydrochloride
    D-Val-Leu-Arg-pNA hydrochloride is a substrate for glandular kinin-releasing enzymes. D-Val-Leu-Arg-pNA hydrochloride can be used to determine the activities of plasminogen activator and plasmin. D-Val-Leu-Arg-pNA hydrochloride is also used to study the fibrinolytic activity of various organisms, such as bacteria and worms.
    D-Val-Leu-Arg-pNA hydrochloride
  • HY-101761R
    TM5441 (Standard)
    		Inhibitor
    TM5441 (Standard) is the analytical standard of TM5441 (HY-101761). This product is intended for research and analytical applications. TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), has IC50 values between 13.9 and 51.1 μM and induces intrinsic apoptosis in several human cancer cell lines. TM5441 attenuates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence.
    TM5441 (Standard)
  • 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-108292R
    Propacetamol hydrochloride (Standard)
    		Inhibitor
    Propacetamol (hydrochloride) (Standard) is the analytical standard of Propacetamol (hydrochloride). This product is intended for research and analytical applications. Propacetamol hydrochloride is a potent, peptidic inhibitor targeting thrombin and granzyme GZMK. Propacetamol hydrochloride specifically blocks the activities of thrombin and GZMK, thereby inhibiting thrombin-mediated PAR-1 cleavage, as well as downstream inflammatory and procoagulant signaling pathways. Through stabilizing IκB proteins, blocking NF-κB activation and reducing systemic levels of proinflammatory/procoagulant biomarkers, Propacetamol hydrochloride exerts multiple effects including anti-inflammatory, antithrombotic, barrier repair, and inhibition of atherosclerotic plaque progression. Propacetamol hydrochloride binds to platelets without interference from kininogen, effectively limiting acute thrombus growth and reducing eosinophil infiltration and goblet cell hyperplasia in asthma models. Propacetamol hydrochloride is an important tool molecule for investigating the mechanisms of atherosclerosis, asthma and related thromboinflammatory diseases.
    Propacetamol hydrochloride (Standard)
  • 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
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