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-124577
    MDI-2268
    		Inhibitor 99.73%
    MDI-2268 is an inhibitor of plasma kallikrein inhibitor 1 (PAI-1). MDI-2268 has good antithrombotic properties and regulates blood coagulation and fibrinolysis process by enhancing fibrinolysis. MDI-2268 can be used in research areas such as deep vein thrombosis.
    MDI-2268
  • HY-122098
    Diaplasinin
    		Inhibitor 99.87%
    Diaplasinin (PAI-749) is a plasminogen activator inhibitor-1 (PAI-1) inhibitor with IC50 of 295 nM. Diaplasinin has antithrombotic efficacy.
    Diaplasinin
  • HY-122714
    SK-216
    		Inhibitor 99.43%
    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-114330A
    ZK824859 hydrochloride
    		Inhibitor 99.03%
    ZK824859 hydrochloride 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 hydrochloride
  • HY-108447
    BC-11 hydrobromide
    		Inhibitor ≥99.0%
    BC-11 hydrobromide is a selective TMPRSS2 inhibitor (TMPRSS2 is a key host cellular factor for viral entry and SARS-CoV-2 pathogenesis), and a selective urokinase (uPA) inhibitor (IC50=8.2 μM). BC-11 hydrobromide is cytotoxic to triple-negative MDA-MB231 breast cancer cells. BC-11 hydrobromide is used in research on viral infections and cancer.
    BC-11 hydrobromide
  • HY-N0518
    Toddalolactone
    		Inhibitor 99.97%
    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
  • HY-150514
    ARN1468
    		Inhibitor 99.34%
    ARN1468 (compound 5) is an orally active and potent serpins inhibitor. ARN1468 can inhibit serpins activity would set the protease free to further reduce prion accumulation. ARN1468 shows anti-prion effect in ScGT1 RML, ScGT1 22L, ScN2a RML, and ScN2a 22L cell lines, with EC50 values of 8.64, 19.3, 11.2, and 6.27 μM.
    ARN1468
  • HY-126361A
    ZK824190 hydrochloride
    		99.61%
    ZK824190 hydrochloride 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 hydrochloride
  • 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-137495
    GGACK
    		Inhibitor
    GGACK (H-Glu-Gly-Arg-CMK) is an irreversible substrate-like serine protease urokinase-type plasminogen activator (uPA) inhibitor.
    GGACK
  • 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-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-135715
    (E)-UK122 TFA
    		Inhibitor
    (E)-UK122 TFA is the isomer of UK122 TFA. UK122 is a potent and selective urokinase-type plasminogen activator (uPA) inhibitor with an IC50 of 0.2 μM.
    (E)-UK122 TFA
  • HY-P4254
    H-Gly-Glu-pNA
    		Substrate
    H-Gly-Glu-pNA is a chromogenic peptide substrate that can be widely used in enzymatic analysis, including trypsin and urokinase-type plasminogen activator (uPA).
    H-Gly-Glu-pNA
  • 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-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-P991340
    CT140
    		Inhibitor
    CT140 is a human IgG4 monoclonal antibody (mAb) targeting PAI-1. Recommend Isotype Controls: Human IgG4 kappa, Isotype Control (HY-P99003).
    CT140
  • HY-122542
    PPACK
    		Inhibitor
    PPACK is potent, selective and irreversible thrombin inhibitor. PPACK can be used an alternative anticoagulant to lithium heparin (LiHep) for blood gas and whole-blood electrolyte analyses. PPACK is also a plasminogen activator (rt-PA) inhibitor. PPACK can inhibit the binding of rt-PA to plasma protease inhibitors.
    PPACK
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Cat. No. Product Name / Synonyms Application Reactivity