1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. PAI-1


Plasminogen activator inhibitor-1 (PAI-1) is the primary inhibitor of tissue-type plasminogen activator (tPA) and urokinase-type plasminogen activator (uPA), and functionally serves to suppress tissue and plasma fibrinolysis.

PAI-1 is a member of the serpin family of proteins and exists in multiple conformations of which a minor component, the “active” form, exhibits inhibitory effects against tPA and uPA.

PAI-1 is an endogenous inhibitor of urokinase-type plasminogen activator (uPA), and its expression is regulated by a number of intrinsic factors (e.g., cytokines and growth factors) and extrinsic factors (e.g., cellular stress).

PAI-1 seems to play a pivotal role in tumor growth and may represent a potential therapeutic target for bladder cancer.

PAI-1 Related Products (9):

Cat. No. Product Name Effect Purity
  • HY-15253
    Tiplaxtinin Inhibitor 98.42%
    Tiplaxtinin is a selective and orally efficacious inhibitor of plasminogen activator inhibitor-1 (PAI-1) with IC50 of 2.7 μM.
  • HY-16511
    Upamostat >98.0%
    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.
  • HY-100447
    TM5275 sodium Inhibitor 98.97%
    TM5275 sodium is a plasminogen activator inhibitor (PAI-1) with an IC50 of 6.95 μM.
  • HY-101761
    TM5441 Inhibitor 98.18%
    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.
  • HY-101214
    UK-371804 Inhibitor >98.0%
    UK-371804 is a urokinase-type plasminogen activator (uPA) inhibitor with a Ki of 10 nM.
  • HY-P2230
    Angstrom6 Inhibitor 99.70%
    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.
  • HY-N1504
    Loureirin B Inhibitor 99.99%
    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.
  • HY-114330A
    ZK824859 hydrochloride Inhibitor
    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.
  • HY-N0518
    Toddalolactone Inhibitor >99.0%
    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.
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