1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. PAI-1

PAI-1 (纤溶酶原激活物抑制物1)

PAI-1 (Plasminogen activator inhibitor-1, also known as SERPINE1) is a member of serine protease inhibitor (SERPIN) family that acts as the primary inhibitor of two main mammalian plasminogen activators, urinary-type (uPA) and tissue-type (tPA). As the main negative regulator of plasminogen activation, PAI-1 is an essential factor in regulation of the physiological balance between thrombosis and fibrinolysis. PAI-1 is a labile molecule that exists in four different forms: active, latent, cleaved and target bound form.

High PAI-1 levels are associated with many cardiovascular diseases. PAI-1 also plays important roles in cell migration, adhesion, senescence, cancer invasion and tissue remodeling. Moreover, the PAI-1 level was extensively validated as the biological prognostic factor in breast cancer and as a marker of a poor prognosis in other cancers. PAI-1 is also one of the plasma biomarkers associated with nonalcoholic fatty liver disease. These associations have made PAI-1 an attractive pharmaceutical target.

PAI-1 相关产品 (13):

目录号 产品名 作用方式 纯度
  • HY-15253
    Tiplaxtinin Inhibitor 98.42%
    Tiplaxtinin 是一种有效的,具有口服活性的选择性的纤溶酶原激活物抑制剂-1 (PAI-1) 抑制剂,IC50 为 2.7 μM。
  • HY-100447
    TM5275 sodium Inhibitor 99.08%
    TM5275 sodium是纤溶酶原激活物抑制剂 (PAI-1),IC50值为6.95 μM。
  • HY-16511
    Upamostat ≥98.0%
    Upamostat (WX-671) 是一种丝氨酸蛋白酶抑制剂。Upamostat 是具有口服活性的 WX-UK1 前药,是一种尿激酶型纤溶酶原激活剂 (uPA) 抑制剂。
  • HY-101214
    UK-371804 Inhibitor ≥98.0%
    UK-371804是尿嘧啶型纤溶酶原激活物 (uPA) 的抑制剂,Ki值为10 nM。
  • HY-N1504
    Loureirin B Inhibitor 99.99%
    Loureirin B 是从剑叶龙血树中分离到的黄酮类化合物,为 PAI-1 的抑制剂,IC50 值为 26.10 μM;Loureirin B 同时可以抑制 KATP,以及 ERKJNK 的磷酸化,具有抗糖尿病的功效。
  • HY-122098
    Diaplasinin Inhibitor
    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。
  • HY-101761
    TM5441 Inhibitor 98.18%
    TM5441 是一种口服生物可利用的纤溶酶原激活物抑制剂-1 抑制剂 (PAI-1),抑制多个癌症细胞系的IC50 值在 13.9 到 51.1 μM,并诱导几种人类癌症细胞的内在调亡。TM5441 减弱 Nω-硝基-1-精氨酸甲酯诱导的心脏高血压和血管衰老。
  • HY-P2230
    Angstrom6 Inhibitor 99.70%
    Angstrom6 (A6 Peptide) 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。
  • HY-100415
    UKI-1 Inhibitor
    UKI-1 (UKI-1C) 是一种有效的尿激酶型纤溶酶原激活剂 (uPA) 抑制剂,Ki 为 0.41 μM。UKI-1 还是一种低分子量的丝氨酸蛋白酶 (serine protease) 抑制剂。UKI-1 是有效的抗转移剂,可抑制癌细胞的侵袭能力。
  • HY-114330A
    ZK824859 hydrochloride Inhibitor 99.19%
    ZK824859 hydrochloride 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 79 nM,1580 nM 和 1330 nM。
  • HY-N0518
    Toddalolactone Inhibitor ≥99.0%
    Toddalolactone,Toddalia asiatica 的主要成分,抑制重组人纤溶酶原激活物抑制物-1 (PAI-1) 的活性, IC50 为 37.31 μM。
  • HY-126361
    ZK824190 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,可用于多发性硬化症的研究。ZK824190 对 uPA,tPA 和 Plasmin 的 IC50 分别为 237,1600 和 1850 nM。
  • HY-114330
    ZK824859 Inhibitor
    ZK824859 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 79 nM,1580 nM 和 1330 nM。
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