| Description | |
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| Catalogue Number | CC4075 |
| Brand Family | Chemicon® |
| Trade Name |
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| Description | Human Plasminogen activator inhibitor-1, recombinant |
| Overview | The sequence corresponding to amino acids 24 to 402 of human PAI-1 (mature form) tagged with 6xHis on the carboxy-terminal was expressed in E. Coli. |
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| Background Information | Plasminogen activator inhibitor-1 (PAI-1) is a member of the serine protease inhibitor (serpin) superfamily and a central regulatory protein in the blood coagulation system. PAI-1 is unique among serpins in exhibiting distinct active and inactive (latent) conformations in vivo. Human PAI-1 is a single-chain glycoprotein with a molecular weight of 43 kDa. This inhibitor acts as "bait" for tissue-type and urokinase-type plasminogen activators (tPA and uPA) and protein C. Its rapid interaction with tPA may function as a major control point in the regulation of fibrinolysis. The highly mobile reactive-center loop (RCL) is thought to account for both the rapid inhibiton of plasminogen activators, and the rapid and spontaneous transition of the unstable, active form of PAI-1 into the stable, inactive conformation (t1/2 at 37oC, 2 hours). The inactive form can be partially reactivated by denaturants such as urea, guanidine hydrochloride or SDS. High concentrations of PAI-1 have been associated with human thromboembolic disease. PAI-1 activity may limit the extent of tumor metastasis, since uPA activity is a major contributory factor promoting dissolution of tumor matrix and basement membrane. |
| Product Information | |
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| Presentation | Liquid. In 150 mm Na2HPO4, pH 6.6, 500 mm NaCl, 2 mm Glutathione, and 0.01% Tween-80. |
| Quality Level | MQ100 |
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| Biological Information | |
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| Purity | >/=98%, as determined by SDS-PAGE gel electrophores. Endotoxin level: < 1EU/microgram. |
| Specific Activity | By uPA activity assay, the recombinant PAI-1 contains a mixture of the active and latent forms, with > 45% of active form. To fully activate the latent PAI-1, the PAI-1 must be incubated in Activation Buffer (2X Activation Buffer: 8 M Guanidine HCl, 40 mm Sodium Acetate, pH 5.6, 400 mm NaCl, 0.2% Tween 20) for 15 to 30 minutes (Sancho, 1994). The recombinant PAI-1 is able to bind to uPA resulting in a SDS-stable complex. |
| Entrez Gene Number |
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| Entrez Gene Summary | Plasminogen activator inhibitor-1 (PAI-1) is the primary, fast-acting inhibitor of plasminogen activators. It is often bound to vitronectin, an abundant component of the extracellular matrix in many tissues. Protease nexin-1 is a potent serpin able to inhibit thrombin, plasmin, and plasminogen activators. PAI-1 and nexin-1 are members of the serpin superfamily and represent clade E. In general, SERine Proteinase INhibitors (serpins) exhibit conformational polymorphism shifting from native to cleaved, latent, delta, or polymorphic forms. Many serpins, such as antitrypsin and antichymotrypsin, function as serine protease inhibitors which regulate blood coagulation cascades. Non-inhibitory serpins perform many diverse functions such as chaperoning proteins or transporting hormones. |
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| UniProt Number |
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| UniProt Summary | FUNCTION: This inhibitor acts as bait for tissue plasminogen activator, urokinase, and protein C. Its rapid interaction with TPA may function as a major control point in the regulation of fibrinolysis. SUBUNIT STRUCTURE: Interacts with VTN. Binds LRP1B; binding is followed by internalization and degradation. SUBCELLULAR LOCATION: Secreted. TISSUE SPECIFICITY: Found in plasma and platelets and in endothelial, hepatoma and fibrosarcoma cells. PTMs: Inactivated by proteolytic attack of the urokinase-type (u-PA) and the tissue-type (TPA), cleaving the 369-Arg-|-Met-370 bond. DISEASE: Defects in SERPINE1 are the cause of plasminogen activator inhibitor-1 deficiency (PAI-1 deficiency) [MIM:173360]. This deficiency is characterized by abnormal bleeding due to SERPINE1 defect in the plasma. High concentrations of SERPINE1 have been associated with thrombophilia [MIM:188050]; an autosomal dominant disorder in which affected individuals are prone to develop serious spontaneous thrombosis. |
| Product Usage Statements | |
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| Usage Statement |
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| Storage and Shipping Information | |
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| Storage Conditions | Store at -80ºC. Thaw on ice and freeze aliquots at -80ºC for longer storage. This product is stable for at least 2 years as supplied. Avoid repeated freeze/thaw cycles. |
| Packaging Information | |
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| Material Size | 50 µg |