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

PAI-1

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.

PAI-1 Related Products (21):

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-100447
    TM5275 sodium
    Inhibitor 99.08%
    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-P2230
    Angstrom6
    Inhibitor 98.77%
    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-100415
    UKI-1
    Inhibitor
    UKI-1 (UKI-1C) 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.
  • HY-120516
    CDE-096
    Inhibitor
    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).
  • HY-14759
    Aleplasinin
    Inhibitor 99.26%
    Aleplasinin is an orally active, potent, BBB-penetrated and selectiveSERPINE1 (PAI-1, Plasminogen activator inhibitor-1) inhibitor. Aleplasinin increases amyloid-β (Aβ) catabolism and ameliorates amyloid-related pathology. Aleplasinin improves memory deficiency. Aleplasinin can be used for Alzheimer's disease research.
  • HY-N10227
    Geodin
    Inhibitor
    Geodin, a fungal metabolite, shows antibacterial activity. Geodin also is an inhibitor of plasminogen activator inhibitor- 1 (PAI-1).
  • 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-128861A
    ACT001
    Inhibitor 99.62%
    ACT001 is an orally active PAI-1 inhibitor by inhibiting the phosphorylation of PI3K and AKT. ACT001 inhibits the phosphorylation of STAT3 and PD-L1 expression by directly binding to STAT3. ACT001, a fumarate salt form of DMAMCL (a prodrug of Micheliolide), can cross the blood-brain barrier. ACT001 exerts synergistic effects in combination with Cisplatin (HY-17394) by inhibiting PI3K/AKT pathway in glioma. ACT001 has potent anti-glioblastoma (GBM) activity and immunomodulatory effects.
  • HY-101214
    UK-371804
    Inhibitor ≥98.0%
    UK-371804 is a urokinase-type plasminogen activator (uPA) inhibitor with a Ki of 10 nM.
  • HY-114330A
    ZK824859 hydrochloride
    Inhibitor 98.77%
    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-N1504
    Loureirin B
    Inhibitor 99.16%
    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-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.
  • 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.
  • HY-122098
    Diaplasinin
    Inhibitor
    Diaplasinin (PAI-749) is a plasminogen activator inhibitor-1 (PAI-1) inhibitor with IC50 of 295 nm. Antithrombotic efficacy.
  • 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.
  • 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.
  • HY-117724
    AZ3976
    Inhibitor
    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.
  • HY-126361A
    ZK824190 hydrochloride
    99.61%
    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.
Isoform Specific Products

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