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

PAI-1 (纤溶酶原激活物抑制物1)

Plasminogen activator inhibitor-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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-108447
    BC-11 hydrobromide Inhibitor 98.50%
    BC-11 hydrobromide 是一种选择性 TMPRSS2 抑制剂 (TMPRSS2 是病毒进入和 SARS-CoV-2 发病机制的关键宿主细胞因子) 和选择性尿激酶 (uPA) 抑制剂 (IC50=8.2 μM)。BC-11 hydrobromide 对三阴性 MDA-MB231 乳腺癌细胞具有细胞毒性。BC-11 hydrobromide 可用于病毒感染和癌症的研究。
    BC-11 hydrobromide
  • HY-117359
    UCD38B hydrochloride Inhibitor
    UCD38B hydrochloride 是一种细胞渗透性、竞争性酶促 uPA 抑制剂,其IC50 值为 7 μM。UCD38B hydrochloride 靶向细胞内 uPA,导致 uPA 错误运输到核周线粒体中,降低线粒体膜电位,随后释放凋亡诱导因子 (AIF)。UCD38B hydrochloride 诱导细胞凋亡 (apoptosis)。
    UCD38B hydrochloride
  • HY-N1533
    28-O-β-D-Glucopyranosyl pomolic acid
    28-O-β-D-Glucopyranosyl pomolic acid 是尿激酶纤溶酶原激活物(uPA)抑制剂,IC50 为 37.82 μM。
    28-O-β-D-Glucopyranosyl pomolic acid
  • HY-122542
    PPACK Inhibitor
    PPACK 是一种纤溶酶原激活剂 (rt-PA) 抑制剂。PPACK 可以抑制纤维蛋白降解产物、纤溶酶原和 α2-抗纤溶酶的变化。PPACK 还可抑制 rt-PA 与血浆蛋白酶抑制剂的结合。
    PPACK
  • HY-P4338
    Glutaryl-Gly-Arg-AMC
    Glutaryl-Gly-Arg-AMC 是尿激酶纤溶酶原激活剂 (uPA) 的肽底物。
    Glutaryl-Gly-Arg-AMC
  • HY-117724
    AZ3976 Inhibitor 98.03%
    AZ3976 是一种有效的纤溶酶原激活物抑制剂 1 型 (PAI-1) 抑制剂,在酶显色分析中 IC50 为 26 μM。在血浆凝块溶解试验中,AZ3976 的IC50 为 16 μM。AZ3976 不与活性 PAI-1 结合,但与潜在 PAI-1 可逆结合。AZ3976 通过增强活性 PAI-1 的潜伏期转换来抑制 PAI-1。AZ3976 在人血浆凝块溶解试验中显示促纤维蛋白溶解活性。
    AZ3976
  • HY-N10227
    Geodin Inhibitor
    Geodin 是一种真菌代谢物,具有抗菌活性。 Geodin 也是纤溶酶原激活物抑制剂-1 (PAI-1) 的抑制剂。
    Geodin
  • HY-137495
    GGACK Inhibitor
    GGACK (H-Glu-Gly-Arg-CMK) 是一种不可逆底物样丝氨酸蛋白酶尿激酶型纤溶酶原激活剂 (uPA) 抑制剂。
    GGACK
  • HY-106508
    Fendosal

    芬度柳

    Inhibitor
    Fendosal (HP 129) 是具有口服活性的、非甾体类的抗炎剂。Fendosal (HP 129) 也是纤溶酶原激活物抑制剂-1 (PAI-1) 的抑制剂。
    Fendosal
  • HY-119160
    TM5007 Inhibitor
    TM5007 是具有口服活性的纤溶酶原激活物抑制剂-1 (PAI-1) 的一种有效抑制剂,其 IC50 值为 29 μM,可增强纤溶活性并抑制凝血。TM5007 还能防止博莱霉素引起的小鼠肺纤维化过程。
    TM5007
  • 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。
    ZK824859
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