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Home >> Signaling Pathways >> Proteases >> PAI-1

PAI-1

Plasminogen activator inhibitor-1 (PAI-1) is the primary inhibitor of tissue-type plasminogen activator (tPA) and urokinase-type plasminogen activator (uPA), and functionally serves to suppress tissue and plasma fibrinolysis.

PAI-1 is a member of the serpin family of proteins and exists in multiple conformations of which a minor component, the “active” form, exhibits inhibitory effects against tPA and uPA.

PAI-1 is an endogenous inhibitor of urokinase-type plasminogen activator (uPA), and its expression is regulated by a number of intrinsic factors (e.g., cytokines and growth factors) and extrinsic factors (e.g., cellular stress).

PAI-1 seems to play a pivotal role in tumor growth and may represent a potential therapeutic target for bladder cancer.

Targets for  PAI-1

Products for  PAI-1

  1. Cat.No. Product Name Information
  2. GC79737 (S)-ZK824859 hydrochloride (S)-ZK824859 hydrochloride is a uPA inhibitor and anticoagulant. (S)-ZK824859 hydrochloride Chemical Structure
  3. GC65281 Aleplasinin

    PAZ-417

     Aleplasinin is an orally active, potent, BBB-penetrated and selectiveSERPINE1 (PAI-1, Plasminogen activator inhibitor-1) inhibitor. Aleplasinin Chemical Structure
  4. GC61511 Angstrom6

    A6 Peptide

     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. Angstrom6 Chemical Structure
  5. GC68013 CDE-096 CDE-096 Chemical Structure
  6. GC79732 D-Val-Leu-Lys-AMC TFA D-Val-Leu-Lys-AMC TFA is a selective fluorogenic peptide substrate of plasmin. D-Val-Leu-Lys-AMC TFA Chemical Structure
  7. GC67781 Diaplasinin

    PAI-749

     Diaplasinin Chemical Structure
  8. GA22381 GGACK (H-Glu-Gly-Arg-chloromethylketone) GGACK (H-Glu-Gly-Arg-chloromethylketone) is an irreversible serine protease inhibitor. GGACK can inhibit urokinase-type plasminogen activator (uPA) and block the plasminogen activation process. GGACK (H-Glu-Gly-Arg-chloromethylketone) Chemical Structure
  9. GA21910 Glutaryl-Gly-Arg-AMC Glutaryl-Gly-Arg-AMC is a fluorescent substrate and a peptide substrate of urokinase plasminogen activator (uPA). The maximum excitation/emission wavelength of the fluorophore AMC is 380nm/460nm. Glutaryl-Gly-Arg-AMC Chemical Structure
  10. GN10267 Loureirin B Loureirin B Chemical Structure
  11. GC79758 PAI-1-IN-1 PAI-1-IN-1 is an orally active and specific PAI-1 inhibitor with an IC50 of <6.95 μM. PAI-1-IN-1 Chemical Structure
  12. GC44671 PPACK

    Pebac, D-Phenylalanyl-prolyl-arginyl Chloromethyl Ketone

     PPACK is a potent selective and irreversible thrombin inhibitor that inhibits human alpha thrombin with a Ki value of 0.24 nM. PPACK Chemical Structure
  13. GC70534 PPACK TFA PPACK TFA is a plasminogen activator (rt-PA) inhibitor. PPACK TFA Chemical Structure
  14. GC12387 Tiplaxtinin(PAI-039)

    PAI-039, Tiplasinin

     Tiplaxtinin(PAI-039) is an orally bioavailable antagonist of plasminogen activator inhibitor-1 (PAI-1) with IC50 value of 2.7μM. Tiplaxtinin(PAI-039) Chemical Structure
  15. GC19358 TM5275 sodium TM5275 sodium is a plasminogen activator inhibitor (PAI-1) with an IC50 of 6.95 uM. TM5275 sodium Chemical Structure
  16. GC18173 TM5441 TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), has IC50 values between 13.9 and 51.1μM and induces intrinsic apoptosis in several human cancer cell lines. TM5441 Chemical Structure
  17. GC38971 Toddalolactone Toddalolactone, a main component of Toddalia asiatica, inhibits the activity of recombinant human plasminogen activator inhibitor-1 (PAI-1), with an IC50 value of 37.31 μM. Toddalolactone Chemical Structure
  18. GC72878 UCD38B hydrochloride UCD38B drochloride is a cell permeant, competitive enzymatic uPA inhibitor with an IC50 value of 7 μM. UCD38B hydrochloride Chemical Structure
  19. GC31889 ZK824859 ZK824859 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. ZK824859 Chemical Structure
  20. GC34324 ZK824859 hydrochloride 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. ZK824859 hydrochloride Chemical Structure

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