Plasminogen Activator Inhibitor-1

Plasminogen activator inhibitor-1 (PAI-1) is encoded by the SERPINE1 gene and is the primary regulator of the plasminogen activation system. High levels of this protein are a risk factor for thrombosis and atherosclerosis, and elevated blood levels are associated with poor clinical outcome and response to therapy in cancer patients.

Products
Background
Literature
Gene Data

Inhibitors

Cat No Product Name / Activity
6187 SK 216
Plasminogen activator inhibitor-1 (PAI-1) inhibitor
5565 Tiplaxtinin
Plasminogen activator inhibitor-1 (PAI-1) inhibitor
5769 TM 5275 sodium salt
Plasminogen activator inhibitor-1 (PAI-1) inhibitor; orally bioavailable
6194 TM 5441
Plasminogen activator inhibitor-1 (PAI-1) inhibitor

Plasminogen activator inhibitor-1 (PAI-1) is a serine protease inhibitor, encoded by the SERPINE1 gene. High levels of this protein are a risk factor for thrombosis and atherosclerosis, and elevated blood levels are associated with poor clinical outcome and response to therapy in cancer patients.

PAI-1 is the primary regulator of the plasminogen activation system, through its inhibitory action on tissue plasminogen activator (tPA) and urokinase (uPA). Both tPA and uPA cleave plasminogen to give plasmin, activating the breakdown of fibrin and matrix metalloproteases (MPPs) which regulate extracellular matrix (ECM) turnover. PAI-1 therefore inhibits fibrinolysis, and regulates tissue homeostasis, wound healing and fibrosis through its inhibition of plasmin mediated MPP activation.

As well as tPA and uPA, PAI-1 binds to vitronectin, an ECM protein that promotes cell adhesion and stabilizes PAI-1 through its binding. It also binds to low-density lipoprotein receptor-related protein (LRP1), promoting cell migration.

Increased levels of PAI-1 are associated with various disease states including obesity, metabolic syndrome, cardiovascular disorders and some forms of cancer. In cancer, pro-tumorigenic factors such as tumor necrosis factor-α (TNFα), transforming growth factor-β (TGFβ) and interleukin-6 (IL-6) stimulate the production of PAI-1 by endothelial cells, fibroblasts and macrophages in the tumor microenvironment. PAI-1 is pro-angiogenic and inhibits spontaneous apoptosis in cancer cells, so is pro-tumorigenic.

Literature for Plasminogen Activator Inhibitor-1

Tocris offers the following scientific literature for Plasminogen Activator Inhibitor-1 to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Cardiovascular

Cardiovascular Research Product Guide

A collection of over 250 products for cardiovascular research, the guide includes research tools for the study of:

  • Hypertension
  • Thrombosis and Hemostasis
  • Atherosclerosis
  • Myocardial Infarction
  • Ischemia/Reperfusion Injury
  • Arrhythmias
  • Heart Failure
Angiogenesis in Cancer

Angiogenesis in Cancer Poster

Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.

Cardiovascular

Cardiovascular Poster

Cardiovascular disease remains one of the major causes of morbidity and mortality in the Western world and therefore this therapeutic area continues to be of great interest to researchers. This poster highlights the key GPCRs regulating vascular reactivity.

Plasminogen Activator Inhibitor-1 Gene Data

Species Gene Symbol Gene Accession No. Protein Accession No.
Human SERPINE1 NM_000602 P05121
Mouse Serpine1 NM_008871 P22777
Rat Serpine1 NM_012620 NP_036752