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 99.97%
    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-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-183626
    TM5614 sodium
    		Inhibitor
    TM5614 sodium is an orally active and specific PAI-1 inhibitor with an IC50 of <6.95 μM. TM5614 sodium blocks the interaction between PAI-1 and serine proteases or LRP-1, and enhances plasmin generation. TM5614 sodium restores macrophage efferocytosis and promotes macrophage polarization. TM5614 sodium alleviates PAI-1-mediated inhibition of Furin, promotes MT1-MMP maturation, activates the NOTCH1 signaling pathway, inhibits proliferation and induces apoptosis. TM5614 sodium promotes skeletal muscle regeneration and alleviates inflammation in a mouse model of skeletal muscle injury. TM5614 sodium can be used in research on skeletal muscle injury-induced inflammation and chronic myeloid leukemia.
    TM5614 sodium
  • HY-123685
    UCD74A hydrochloride
    		Inhibitor
    UCD74A (compound 18) hydrochloride is a 5-substituted amiloride analog and urokinase-type plasminogen activator (uPA) inhibitor with an IC50 of 110 μM.UCD74A (hydrochloride) modulates plasminogen activation cascades linked to extracellular matrix remodeling.UCD74A (hydrochloride) can be used for the research of tumor metastasis.
    UCD74A hydrochloride
  • 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-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-100447
    TM5275 sodium
    		Inhibitor 98.97%
    TM5275 sodium can inhibit the interaction between PAI-1 and LRP1.
    TM5275 sodium
  • HY-132187
    Sphingosylphosphorylcholine
    		99.50%
    Sphingosylphosphorylcholine is a bioactive lipid and a major component of plasma high-density lipoprotein that binds to OGR1 with a Kd of 33.3 nM. Sphingosylphosphorylcholine triggers delayed phosphorylation of Smad2, upregulates α-SMA expression, and activates TRPM3. Sphingosylphosphorylcholine reduces Apoptosis and upregulates the expression of uPA and its receptor uPA-R. Sphingosylphosphorylcholine exerts anti-apoptotic, anti-cardiac hypertrophy and pro-wound healing effects. Sphingosylphosphorylcholine induces scratching behavior in mice. Sphingosylphosphorylcholine is used in studies related to atopic dermatitis, promyelocytic leukemia, heart failure, myocardial ischemia/reperfusion injury, ovarian cancer, breast cancer, pancreatic cancer, and skin wound healing disorders in genetically impaired healing diabetes.
    Sphingosylphosphorylcholine
  • HY-16511
    Upamostat
    		99.02%
    Upamostat (WX-671), a prodrug of WX-UK1, is an orally active serine protease inhibitor. Upamostat 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 can be used in the research of metastatic breast cancer and locally advanced pancreatic cancer.
    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-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-N1504
    Loureirin B
    		Inhibitor 99.96%
    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-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-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-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-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-101214
    UK-371804
    		Inhibitor 98.0%
    UK-371804 is a urokinase-type plasminogen activator (uPA) inhibitor with a Ki of 10 nM.
    UK-371804
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity