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-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-N3097R
    Pellitorine (Standard)
    		Inhibitor
    Pellitorine (Standard) is the analytical standard of Pellitorine (HY-N3097). 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 (Standard)
  • 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-137495A
    GGACK hydrochloride
    		Inhibitor
    GGACK (H-Glu-Gly-Arg-CMK) hydrochloride is an irreversible substrate-like serine protease urokinase-type plasminogen activator (uPA) inhibitor.
    GGACK hydrochloride
  • HY-155607
    APC8696
    APC8696 is a reversible uPA inhibitor, with a Ki of 8 nM.
    APC8696
  • 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-181993
    JNK3-IN-11
    JNK3-IN-11 is a selective JNK3 inhibitor with an IC50 of 2.08 nM. JNK3-IN-11 binds to the JNK3 ATP-binding pocket, forming conserved hydrogen bonds with Met149 and a water-mediated hydrogen bond with Lys93. JNK3-IN-11 suppresses TGF-β1-induced c-Jun phosphorylation, reduces profibrotic markers COL1A1 and PAI-1, restores E-cadherin expression, and has protection against podocyte injure. JNK3-IN-11 can be used for the research of chronic kidney disease.
    JNK3-IN-11
  • 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-P992313
    AS3288802
    		Inhibitor
    AS3288802, a highly selective active plasminogen activator inhibitor-1 (PAI-1) antibody, is a PAI-1 inhibitor with a human IC50 and EC50 values of 4.2 ng/mL. AS3288802 can be used for the research of thrombosis and fibrosis-related diseases.
    AS3288802
  • HY-W701541
    6-Aminocaproic acid-d10 hydrochloride
    6-Aminocaproic acid-d10 hydrochloride (EACA-d10 hydrochloride; Epsilon-Amino-n-caproic Acid-d10 hydrochloride; 6-Aminohexanoic acid-d10 hydrochloride) is the deuterium labeled 6-Aminocaproic acid hydrochloride (HY-B0236A). 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-d<sub>10</sub> hydrochloride
  • 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 a potent, peptidic inhibitor targeting thrombin and granzyme GZMK. PPACK 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, PPACK exerts multiple effects including anti-inflammatory, antithrombotic, barrier repair, and inhibition of atherosclerotic plaque progression. PPACK binds to platelets without interference from kininogen, effectively limiting acute thrombus growth and reducing eosinophil infiltration and goblet cell hyperplasia in asthma models. PPACK is an important tool molecule for investigating the mechanisms of atherosclerosis, asthma and related thromboinflammatory diseases.
    PPACK
  • HY-P10878
    UK140
    UK140 is the inhibitor for urokinase-type plasminogen activator (uPA) with Ki of 0.20 µM and 2.79 µM for huPA anf muPA. UK140 can be used in metastasis-related research.
    UK140
  • HY-N7128R
    Flavanone (Standard)
    		Activator
    Flavanone (Standard) is the analytical standard of Flavanone. This product is intended for research and analytical applications. Flavanone is a naturally occurring flavone. Flavanone has inhibitory activity for human estrogen synthetase (aromatase). lavanone is the inhibitor for ERK/p38/NF-κB signaling pathway. Flavanone exhibits oral activity and antitumor efficacy.
    Flavanone (Standard)
  • HY-114150
    D-Val-Leu-Arg-pNA
    D-Val-Leu-Arg-pNA is a glandular kininoreleasing enzyme substrate that also acts as a substrate for tissue-type plasminogen activator (t-PA) with no apparent affinity for fibrin.
    D-Val-Leu-Arg-pNA
  • HY-P992410
    MEDI-579
    		Inhibitor
    MEDI-579 is a fully human monoclonal antibody against PAI-1, with a KD value of 6 pM for human PAI-1 and 105 pM for rat PAI-1. MEDI-579 restores renal plasmin activity and inhibits PAI-1-mediated intracellular signal transduction. MEDI-579 reduces albuminuria, glomerulosclerosis severity, TGF-β1 expression level, and phosphorylated Smad2 level induced in diabetic mice. MEDI-579 decreases the levels of active PAI-1 in plasma and kidneys, and increases plasma plasmin level in a mouse model of lupus nephritis. MEDI-579 can be used in research related to diabetic nephropathy and lupus nephritis. The recommended isotype control is human IgG1 kappa (HY-P99001).
    MEDI-579
  • HY-173272
    BT-114143
    BT-114143 is a plasminogen activation inhibitor, with an IC50 of 8.42 μM. BT-114143 can be used in the research of hemorrhagic diseases caused by hyperfibrinolysis, such as traumatic bleeding, severe menstrual bleeding, postpartum hemorrhage, and complications of hemophilia.
    BT-114143
  • HY-N18088
    2-O-(2,4,6-Trihydroxyphenyl)-6,6'-bieckol
    2-O-(2,4,6-Trihydroxyphenyl)-6,6'-bieckol (Compound 4) is a bispolyphenol. 2-O-(2,4,6-Trihydroxyphenyl)-6,6'-bieckol can be isolated from the brown alga Ecklonia kurome OKAMURA. 2-O-(2,4,6-Trihydroxyphenyl)-6,6'-bieckol exhibits inhibitory activities toward both α2-macroglobulin (α-M) and α-PI, with IC50s of 1.9 μg/mL and 0.7 μg/mL, respectively.
    2-O-(2,4,6-Trihydroxyphenyl)-6,6'-bieckol
  • HY-106508
    Fendosal
    		Inhibitor 99.82%
    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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity