PAI-1 Inhibitor

Tiplaxtinin is a selective and orally efficacious inhibitor of plasminogen activator inhibitor-1 (PAI-1) with IC₅₀ of 2.7 μM.

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.

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.

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.

PAI-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.

Mito-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.

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.

TM5275 sodium can inhibit the interaction between PAI-1 and LRP1.

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.

UKI-1 (WX-UK1) is a potent urokinase-type plasminogen activator (uPA) inhibitor with a K_i 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.

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 K_ATP, the phosphorylation of ERK and JNK, and has anti-diabetic activity.

4-Aminobenzamidine (p-Aminobenzamidine) dihydrochloride is a strong trypsin inhibitor. 4-Aminobenzamidine dihydrochloride acts as an orally active urokinase type plasminogen activator (uPA) inhibitor (K_i=82 μM). 4-Aminobenzamidine dihydrochloride can be used for cardiovascular diseases and anti-tumor study.

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.

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.

UK-371804 is a urokinase-type plasminogen activator (uPA) inhibitor with a K_i of 10 nM.

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.

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).

Diaplasinin (PAI-749) is a plasminogen activator inhibitor-1 (PAI-1) inhibitor with IC₅₀ of 295 nM. Diaplasinin has antithrombotic efficacy.

Pegevongitide (AV-001) is a Tie2 agonist. Pegevongitide resists the increased endothelial cell permeability induced by SARS-CoV-2 infection. Pegevongitide activates the angiogenin (angiogenin)/Tie2 signaling pathway. Pegevongitide reduces perivascular space dilation and upregulates perivascular Aquaporin-4 expression. Pegevongitide decreases the expression of TNF-α, PAI-1, CXCL9 and P-selectin, improves white matter integrity, enhances cognitive function and exerts neuroprotective effects. Pegevongitide improves white matter integrity in middle-aged rats with vascular dementia induced by multiple microinfarctions. Pegevongitide can be used in related research on diseases such as COVID-19 and vascular dementia.

Stromab (DS9231) is a human IgG1 monoclonal antibody (mAb) targeting Serpin F2. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001).