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

PAI-1(纤溶酶原激活物抑制物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.

Products for  PAI-1

  1. Cat.No. 产品名称 Information
  2. GC65281 Aleplasinin

    PAZ-417

     Aleplasinin 是一种口服有效的、可透过血脑屏障的、选择性的 SERPINE1 (PAI-1，纤溶酶原激活物抑制剂 -1) 抑制剂。Aleplasinin 增加淀粉样蛋白 -β (Aβ) 分解代谢，改善淀粉样蛋白相关病理。Aleplasinin 可改善记忆缺陷。Aleplasinin 可用于阿尔茨海默病的研究。
  3. GC61511 Angstrom6

    A6 Peptide

     Angstrom6(A6Peptide)是一种来源于单链尿激酶纤溶酶原激活剂(scuPA)的8个氨基酸的肽，可干扰uPA/uPAR级联反应并消除下游效应。Angstrom6与CD44结合，抑制肿瘤细胞的迁移、侵袭和转移，调节CD44介导的细胞信号。
  4. GC68013 CDE-096 CDE-096 是一种有效的 PAI-1 抑制剂。CDE-096 可防止PAI-1 以类似的效力 (分别为 IC50=30 和25 nM) 使 tPA 和 uPA 失活，并对糖基化 PAI-1 以及来源于几种物种的 PAI-1 具有活性 (对小鼠、大鼠和猪 PAI-1 分别为 IC50=19、22 和 18 nM)。
  5. GC67781 Diaplasinin

    PAI-749

     Diaplasinin (PAI-749) 是纤溶酶原激活剂抑制剂-1 (PAI-1) 抑制剂，IC50 为 295 nm。具有抗血栓功效。
  6. GN10267 Loureirin B

    龙血素 B

     A flavonoid with diverse biological activities
  7. GC70534 PPACK TFA PPACK TFA是一种纤溶酶原激活剂(rt-PA)抑制剂。
  8. GC12387 Tiplaxtinin(PAI-039)

    ALPHA-氧代-1-(苯基甲基)-5-[4-(三氟甲氧基)苯基]-1H-吲哚-3-乙酸,PAI-039; Tiplasinin

     A PAI-1 inhibitor
  9. GC19358 TM5275 sodium A PAI-1 inhibitor
  10. GC18173 TM5441 A PAI-1 inhibitor
  11. GC38971 Toddalolactone

    毛两面针素

     Toddalolactone, a natural coumarin, inhibits the activity of recombinant human Plasminogen activator inhibitor-1 (PAI-1) in a dose-dependent manner, yielding an IC50 value of 37.31 ± 3.23 μM.
  12. GC31889 ZK824859 ZK824859 is a potent, selective and orally bioavailable inhibitor of urokinase plasminogen activator (uPA) with IC50 of 79?nM, 1580?nM and 1330?nM for human uPA, tPA, and plasmin, respectively.
  13. GC34324 ZK824859 hydrochloride ZK824859hydrochloride是一种口服有效的选择性尿激酶型纤溶酶原激活剂(uPA)抑制剂，用于人uPA，tPA和纤溶酶，IC50分别为79nM，1580nM和1330nM。

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