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 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-101214
    UK-371804
    		Inhibitor 98.0%
    UK-371804 is a urokinase-type plasminogen activator (uPA) inhibitor with a Ki of 10 nM.
    UK-371804
  • HY-108447
    BC-11 hydrobromide
    		Inhibitor 99.22%
    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-P4338
    Glutaryl-Gly-Arg-AMC
    		99.24%
    Glutaryl-Gly-Arg-AMC is a peptide substrate of urokinase plasminogen activator (uPA).
    Glutaryl-Gly-Arg-AMC
  • HY-116868
    Anecortave acetate
    		Activator 99.81%
    Anecortave acetate is a potent ocular angiostatic agent. Anecortave acetate inhibits neovascularization which is induced by many different angiogenic factors, and increases plasminogen activator inhibitor-1 (PAI-1) mRNA expression. Anecortave acetate can be used to research ocular neovascular diseases.
    Anecortave acetate
  • HY-120516
    CDE-096
    		Inhibitor 99.98%
    CDE-096 is a potent inhibitor of PAI-1. CDE-096 prevents PAI-1 from inactivating tPA and uPA with similar potency (IC50=30 and 25 nM, respectively) and is active against glycosylated PAI-1, as well as PAI-1 derived from several species (IC50=19, 22 and 18 nM for murine, rat, and Porcine PAI-1, respectively).
    CDE-096
  • 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-P991422
    Stromab
    		Inhibitor 99.28%
    Stromab (DS9231) is a human IgG1 monoclonal antibody (mAb) targeting Serpin F2. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001).
    Stromab
  • HY-P4341A
    D-Val-Leu-Lys-AMC TFA
    		Substrate 99.65%
    D-Val-Leu-Lys-AMC TFA is a selective fluorogenic peptide substrate of plasmin. D-Val-Leu-Lys-AMC TFA can be used for the quantification of enzymatic activity of plasmin. Ex: 360-380 nm, Em: 440-460 nm.
    D-Val-Leu-Lys-AMC TFA
  • HY-126361A
    ZK824190 hydrochloride
    		99.42%
    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-N3097
    Pellitorine
    		Inhibitor 99.84%
    Pellitorine is a bioactive natural amide compound. Pellitorine can competitively antagonize the activation of TRPV1 by Capsaicin (HY-10448), thereby reducing pain signal transmission. Pellitorine improves cognitive dysfunction by upregulating the BDNF-ERK1/2-CREB and Nrf2-HO-1 pathways. Pellitorine exerts anti-inflammatory and anti-sepsis effects by inhibiting the release of high mobility group protein B1 (HMGB1) and the expression of RAGE/TLR4. Pellitorine exerts its antithrombotic effect by prolonging the clotting time, inhibiting the activity of clotting factors and thrombin. Pellitorine inhibits lipid peroxidation and resists ferroptosis by upregulating GPX4 and DHODH. Pellitorine kills Aedes aegypti mosquito larvae by inhibiting V-type H⁺-ATPase and aquaporin 4 (AaAQP4). Pellitorine exhibits anti-cancer activity (e.g., leukemia and breast cancer) and has inhibitory effects on certain bacteria.
    Pellitorine
  • 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-117724
    AZ3976
    		Inhibitor 98.05%
    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-165084
    L-a-Phosphatidylserine sodium
    		Activator 99.0%
    L-α-Phosphatidylserine sodium (Soy PS sodium) is a negatively charged phospholipid that acts as an allosteric activator to activate latent plasminogen activator inhibitor-1 (PAI-1). L-α-Phosphatidylserine does not directly alter the catalytic activity of t-PA, but regulates fibrinolytic activity solely by inducing conformational remodeling of PAI-1. L-α-Phosphatidylserine sodium is an antigen targeting phosphatidylserine (PS) and can induce the production of polyclonal antibodies. L-α-Phosphatidylserine is mainly used in studies related to immunology, fibrinolytic system and coagulation homeostasis.
    L-a-Phosphatidylserine sodium
  • HY-P10877
    Bicyclic UK18
    		98.14%
    Bicyclic UK18 is a competitive inhibitor for human urokinase-type plasminogen activator (uPA) with a Ki of 53 nM.
    Bicyclic UK18
  • 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-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-132187S1
    Sphingosylphosphorylcholine-d7
    		99.90%
    Sphingosylphosphorylcholine-d7 is the deuterium labeled Sphingosylphosphorylcholine (HY-132187).
    Sphingosylphosphorylcholine-d<sub>7</sub>
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity