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

PAI-1 Inhibitor

PAI-1 Inhibitors (46):

Cat. No. Product Name Effect Purity
  • HY-15253
    Tiplaxtinin
    		Inhibitor 99.33%
    Tiplaxtinin is a selective and orally efficacious inhibitor of plasminogen activator inhibitor-1 (PAI-1) with IC50 of 2.7 μM.
  • 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.
  • 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.
  • 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.
  • 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.
  • HY-123685
    UCD74A (hydrochloride)
    		Inhibitor
    UCD74A hydrochloride is a 5-substituted Amiloride (HY-B0285) 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.
  • 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.
  • HY-100447
    TM5275 sodium
    		Inhibitor 98.97%
    TM5275 sodium can inhibit the interaction between PAI-1 and LRP1.
  • 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.
  • 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.
  • 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.
  • 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.
  • 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.
  • HY-101214
    UK-371804
    		Inhibitor 98.0%
    UK-371804 is a urokinase-type plasminogen activator (uPA) inhibitor with a Ki of 10 nM.
  • HY-122714
    SK-216
    		Inhibitor 99.43%
    SK-216 is a plasminogen activator inhibitor-1 (PAI-1) inhibitor that acts as an anti-metastatic agent for human osteosarcoma and inhibits lung metastasis of human osteosarcoma.
  • HY-108447
    BC-11 hydrobromide
    		Inhibitor 99.22%
    BC-11 hydrobromide is a selective TMPRSS2 inhibitor (TMPRSS2 is a key host cellular factor for viral entry and SARS-CoV-2 pathogenesis), and a selective urokinase (uPA) inhibitor (IC50=8.2 μM). BC-11 hydrobromide is cytotoxic to triple-negative MDA-MB231 breast cancer cells. BC-11 hydrobromide is used in research on viral infections and cancer.
  • HY-120516
    CDE-096
    		Inhibitor 99.98%
    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-122098
    Diaplasinin
    		Inhibitor 99.87%
    Diaplasinin (PAI-749) is a plasminogen activator inhibitor-1 (PAI-1) inhibitor with IC50 of 295 nM. Diaplasinin has antithrombotic efficacy.
  • HY-P991422
    Stromab
    		Inhibitor 99.28%
    Stromab (DS9231) is a human IgG1 monoclonal antibody (mAb) targeting Serpin F2. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001).
  • HY-N3097
    Pellitorine
    		Inhibitor 99.84%
    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.