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  2. Integrin


Integrins, a family of heterodimeric adhesion receptors for diverse extracellular matrices, have consistently been implicated as crucial drivers of ovarian cancer development and progression. A number of the RGD-based members of the integrin family, including α5β1, and αvβ3 or αvβ5 integrins, are markedly elevated in aggressive ovarian tumors. These adhesion receptors appear to promote cell adhesion, survival, motility and invasion during ovarian tumor growth or metastatic progression. Importantly, the functions of these integrins are strongly dependent on the activation of focal adhesion kinase (FAK) and its downstream signaling, including the PI3K/Akt- and Ras/MAPK-dependent pathways.

Integrins are transmembrane proteins and are major receptors for cell-extracellular matrix (ECM) and cell-cell adhesion. Modulation of these molecules, particularly αv integrin family, has exhibited profound effects on fibrosis in multiple organ and disease state. Based on the several studies, the integrins αvβ3, αvβ5, αvβ6, and αvβ8 have been known to modulate the fibrotic process via activation of latent transforming growth factor (TGF)-β in pre-clinical models of fibrosis.

Each integrin is typically formed by the non-covalent pairing of one α subunit, of which, 18 types are known to exist, and one β subunit, of which 8 types are known to exist. Together, 24 distinct heterodimers have been identified to date. The αv subunit can form heterodimers with the β1, β3, β5, β6 or β8 subunits and β1 can associate with many different α subunits from α1 to α11, and αv, indicating that not all theoretically possible α and subunit pairs form. Interestingly, the activation of TGF-β appears to be a common function of multiple αv integrins.

Integrin 相关产品 (26):

Cat. No. Product Name Effect Purity
  • HY-16141
    Cilengitide Inhibitor 99.04%
    Cilengitide 是一种有效的选择性integrin αvβ3 和 αvβ5 受体抑制剂,抑制离体的 αvβ3 和 αvβ5 结合到玻璃粘连蛋白,IC50 分别为 4 和 79 nM。
  • HY-12290
    Arg-Gly-Asp-Ser Inhibitor >98.0%
    Arg-Gly-Asp-Ser 是一种整合素受体 (integrin receptor) 抑制剂,能够降低炎症性细胞因子的表达,从而减少全身炎症的发生。
  • HY-P0023
    Cyclo(-RGDfK) Inhibitor >98.0%
  • HY-18644
    CWHM-12 Inhibitor 98.97%
    CWHM-12 是一种有效的 αV integrins 抑制剂,抑制 αvβ8αvβ3αvβ6αvβ1IC50 分别为 0.2,0.8,1.5 和 1.8 nM。
  • HY-13535A
    ATN-161 trifluoroacetate salt Antagonist
    ATN-161 trifluoroacetate salt 是一种新型 integrin α5β1 拮抗剂,在肝转移模型小鼠模型中,抑制血管生成。
  • HY-P9911
    Vedolizumab Antagonist
    Vedolizumab是一种靶向α4β7整联蛋白 (integrin) 的人源化单克隆抗体,用来治疗溃疡性结肠炎和克罗恩病。
  • HY-U00235
    SR121566A Antagonist
    SR121566A 是一种新型的非肽 Glycoprotein IIb/IIIa (GP IIb-IIIa) 拮抗剂,可以抑制 ADP,花生四烯酸和胶原诱导的人血小板集合,IC50s 分别为 46±7.5,56±6 和 42±3 nM。
  • HY-P0290
    GRGDSP Inhibitor
    GRGDSP 是一种合成的线性RGD肽,是一种整联蛋白 (integrin) 抑制剂。
  • HY-14951
    Firategrast Antagonist 99.66%
    Firategrast 是一种口服 α4β1/α4β7 整合素拮抗剂。
  • HY-14571
    E7820 Inhibitor 98.36%
    E7820 是一种血管生成抑制剂,能够抑制整合素蛋白 a2 (integrin a2) 的活性,整合素蛋白 a2 是内皮细胞中的细胞粘附分子。
  • HY-18676
    OSU-T315 Inhibitor 99.42%
    OSU-T315 是一种新型的ILK抑制剂, IC50值为0.6 μM。
  • HY-19767A
    Integrin Antagonist 1 hydrochloride Antagonist 99.87%
    Integrin Antagonist 1盐酸盐是一种小分子整联蛋白αvβ6拮抗剂,在荧光偏振检测中对人a 6蛋白亲和力(pIC 50)为8.1,在细胞粘连检测中,其亲合性分别为:ανβ6 (pIC50 = 8.4); ανβ3 (pIC50 = 6); ανβ5 (pIC 50 = 6.9); ανβ8 (pIC50 = 7.7)。
  • HY-B0686
    Eptifibatide Inhibitor 99.18%
  • HY-100506
    GLPG0187 Antagonist 98.08%
    GLPG0187是广谱的integrin受体拮抗剂,具有抗肿瘤活性;抑制αvβ1-integrin的IC50值为1.3 nM。
  • HY-17369
    Tirofiban hydrochloride monohydrate Antagonist >98.0%
  • HY-N0416
    Cucurbitacin B Inhibitor 99.36%
    葫芦素B (Cucurbitacin B)是一具有抗癌活性的天然化合物。
  • HY-19344
    Lifitegrast Antagonist 99.12%
    Lifitegrast是整合素淋巴细胞功能相关抗原-1(LFA-1)的拮抗剂; 抑制Jurkat T细胞附着于ICAM-1IC50为2.98nM。
  • HY-13535
    ATN-161 Antagonist
    ATN-161 (Ac-PHSCN-NH2)是一由纤连蛋白的协同区域衍生出的五氨基酸短肽;具有抗肿瘤活性的β整合素拮抗剂。
  • HY-70073
    Zaurategrast Inhibitor 98.55%
    Zaurategrast 是一种口服有效的 α4-integrin 抑制剂。
  • HY-15770
    TR-14035 Antagonist
    TR-14035是α4β7/α4β1 integrin拮抗剂,IC50为7 nM和87 nM。