PAI-1 Inhibitor
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6-Aminocaproic acid
0 ImagesSynonyms: EACA; Epsilon-Amino-n-caproic Acid; 6-Aminohexanoic acid6-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.
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TM5441
0 ImagesTM5441 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.
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Angstrom6
0 ImagesSynonyms: A6 PeptideAngstrom6 (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.
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PAI-1-IN-1
0 ImagesPAI-1-IN-1 is an orally active and specific PAI-1 inhibitor with an IC50 of <6.95 μM. PAI-1-IN-1 blocks the interaction between PAI-1 and serine proteases or LRP-1, and enhances plasmin generation. PAI-1-IN-1 restores macrophage efferocytosis and promotes macrophage polarization. PAI-1-IN-1 alleviates PAI-1-mediated inhibition of Furin, promotes MT1-MMP maturation, activates the NOTCH1 signaling pathway, inhibits proliferation and induces apoptosis. PAI-1-IN-1 promotes skeletal muscle regeneration and alleviates inflammation in a mouse model of skeletal muscle injury. PAI-1-IN-1 can be used in research on skeletal muscle injury-induced inflammation and chronic myeloid leukemia.
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Mito-Esculetin
0 ImagesCat. No.: HY-184265CAS No.: 1993461-76-9Synonyms: Mito-EscMito-Esculetin (Mito-Esc) is an orally active mitochondria-targeted derivative of Esculetin (HY-N0284). Mito-Esculetin inhibits LPS-induced phosphorylation of STAT3 Tyr-705, partially reverses LPS-mediated depletion of SIRT3, and enhances the AMPK-SIRT1 signaling axis. Mito-Esculetin inhibits PAI-1 activity, regulates miRNA, and induces phosphorylation of IRS and AKT. Mito-Esculetin suppresses oxidant-induced endothelial dysfunction, Ang-II (HY-13948)- and high glucose-induced atherosclerotic plaque formation, Palmitate (HY-N0830)-induced insulin resistance, as well as high glucose-mediated endothelial cell senescence and inflammatory responses. Mito-Esculetin reduces body weight and non-esterified fatty acid (NEFA) levels. Mito-Esculetin can be used in research related to acute coronary syndrome, type 2 diabetes, and hyperglycemia-induced atherosclerosis.
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UCD74A (hydrochloride)
0 ImagesCat. No.: HY-123685CAS No.: 1345838-99-4UCD74A 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.
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Aleplasinin
0 ImagesSynonyms: PAZ-417Aleplastinin (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.
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MDI-2268
0 ImagesMDI-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.
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UKI-1
0 ImagesCat. No.: HY-100415CAS No.: 220355-63-5Synonyms: WX-UK1; UKI-1CUKI-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.
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4-Aminobenzamidine dihydrochloride
0 ImagesSynonyms: p-Aminobenzamidine dihydrochloride4-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.
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ZK824859 hydrochloride
0 ImagesZK824859 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.
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UK-371804
0 ImagesUK-371804 is a urokinase-type plasminogen activator (uPA) inhibitor with a Ki of 10 nM.
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BC-11 hydrobromide
0 ImagesBC-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.
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CDE-096
0 ImagesCDE-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).
