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-15253
    Tiplaxtinin
    		Inhibitor 99.03%
    Tiplaxtinin is a selective and orally efficacious inhibitor of plasminogen activator inhibitor-1 (PAI-1) with IC50 of 2.7 μM.
    Tiplaxtinin
  • HY-P2373
    Kinase, Natto fermentation
    Kinase, Natto fermentation is a potent fibrinolytic enzyme. Kinase, Natto fermentation can break down blood clots by directly hydrolyzing fibrin and plasmin substrate. Kinase, Natto fermentation can be used for the research of cardiovascular diseases.
    Kinase, Natto fermentation
  • HY-B0236
    6-Aminocaproic acid
    		Inhibitor 99.86%
    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
  • HY-101761
    TM5441
    		Inhibitor 99.08%
    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
  • HY-122542B
    PPACK TFA
    		Inhibitor 99.80%
    PPACK TFA is potent, selective and irreversible thrombin inhibitor. PPACK TFA can be used an alternative anticoagulant to lithium heparin (LiHep) for blood gas and whole-blood electrolyte analyses. PPACK TFA is also a plasminogen activator (rt-PA) inhibitor. PPACK TFA can inhibit the binding of rt-PA to plasma protease inhibitors.
    PPACK TFA
  • 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-P991422
    Stromab
    		Inhibitor
    Stromab (DS9231; TS-23; CSL-301) is a human IgG1 monoclonal antibody (mAb) targeting Serpin F2. Stromab can be used in schaemic stroke, Pulmonary embolism, Myocardial infarction and Thrombosis research. Recommended isotype control: Human IgG1 lambda, Isotype Control (HY-P99992).
    Stromab
  • 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-P2230
    Angstrom6
    		Inhibitor 99.98%
    Angstrom6 (A6 Peptide) is an 8 amino-acid peptide derived from single-chain urokinase plasminogen activator (scuPA) and interferes with the uPA/uPAR cascade and abrogates downstream effects. Angstrom6 binds to CD44 resulting in the inhibition of migration, invasion, and metastasis of tumor cells, and the modulation of CD44-mediated cell signaling.
    Angstrom6
  • HY-100447
    TM5275 sodium
    		Inhibitor 98.97%
    TM5275 sodium is a plasminogen activator inhibitor (PAI-1) with an IC50 of 6.95 μM.
    TM5275 sodium
  • HY-14759
    Aleplasinin
    		Inhibitor 99.59%
    Aleplastinin (PAZ-417) is an orally active, blood-brain barrier permeable, selective SERPINE1 (PAI-1) inhibitor (IC50=655 nM). Aleplastinin activates the tissue type plasminogen activator (tPA)/fibrinolysis cascade by inhibiting PAI-1, thereby promoting the degradation of amyloid-β (Aβ) oligomers and monomers. Aleplastinin can significantly reduce plasma and brain Aβ levels, improve memory impairment, and reverse cognitive impairment. Aleplastinin can be used for research on Alzheimer's disease.
    Aleplasinin
  • HY-16511
    Upamostat
    		99.02%
    Upamostat (WX-671) is a serine protease inhibitor. Upamostat is the orally available prodrug of the WX-UK1, which is a urokinase plasminogen activator (uPA) inhibitor.
    Upamostat
  • HY-100415
    UKI-1
    		Inhibitor
    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
  • 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-W018723
    4-Aminobenzamidine dihydrochloride
    		Inhibitor 99.97%
    4-Aminobenzamidine (p-Aminobenzamidine) dihydrochloride is a strong trypsin inhibitor. 4-Aminobenzamidine dihydrochloride acts as an orally active urokinase type plasminogen activator (uPA) inhibitor (Ki=82 μM). 4-Aminobenzamidine dihydrochloride can be used for cardiovascular diseases and anti-tumor study.
    4-Aminobenzamidine dihydrochloride
  • HY-46749
    Muvalaplin tetrahydrochloride
    		99.55%
    Muvalaplin tetrahydrochloride (LY3473329) is an orally active reagent of lipoprotein (a) (Lp (a)). At present, research on Muvalaplin tetrahydrochloride oral reagent is ongoing.
    Muvalaplin tetrahydrochloride
  • HY-N7128
    Flavanone
    		Activator 99.73%
    Flavanone is a naturally occurring flavone. Flavanone has inhibitory activity for human estrogen synthetase (aromatase). Flavanone is the inhibitor for ERK/p38/NF-κB signaling pathway. Flavanone exhibits oral activity and antitumor efficacy.
    Flavanone
  • HY-N1504
    Loureirin B
    		Inhibitor 99.95%
    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
  • 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-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
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Cat. No. Product Name / Synonyms Application Reactivity