1. Signaling Pathways
  2. Cytoskeleton
  3. 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 (57):

Cat. No. Product Name Effect Purity
  • HY-16141
    Cilengitide Inhibitor 99.06%
    Cilengitide 是含RGD的环肽。Cilengitide 是有效,选择性的αvβ3 和αvβ5受体整合素抑制剂,IC50分别为4和79 nM。
  • HY-P0023
    Cyclo(-RGDfK) Inhibitor >98.0%
    Cyclo(-RGDfK) 是有效,选择性的整合素 αvβ3 抑制剂,其 IC50 值为 0.94 nM。
  • HY-18644
    CWHM-12 Inhibitor 99.65%
    CWHM-12是αV整联蛋白的有效抑制剂,抑制αvβ8αvβ3αvβ6αvβ1IC50 值分别为0.2,0.8,1.5,1.8 nM。
  • HY-P0122
    iRGD peptide 98.62%
    iRGD peptide 是一种由 9 个氨基酸组成的环肽,先与 av integrins 结合,随后酶解产生 CRGDK/R 与 神经纤毛蛋白-1 (neuropilin-1) 相互作用,从而促进药物的组织渗透,具有靶向肿瘤、肿瘤渗透的作用。
  • HY-18676
    OSU-T315 Inhibitor 99.88%
    OSU-T315 是整联蛋白连接激酶 (ILK) 的抑制剂 (IC50=0.6 μM), 通过去磷酸化 AKT-Ser473 和其他 ILK 靶标 (GSK-3β和肌球蛋白轻链) 抑制 PI3K/AKT 信号传导。 OSU-T315 阻止 AKT 转位到脂筏消除 AKT 的活化,并以 ILK 非依赖性方式触发 Caspase 依赖性细胞凋亡 (Apoptosis)。OSU-T315 通过自噬 (Autophagy) 和凋亡 (Apoptosis) 导致细胞死亡。
  • HY-111413A
    c(phg-isoDGR-(NMe)k) TFA
    c(phg-isoDGR-(NMe)k) TFA 是有效选择性的 α5β1 整合素配体,IC50 为 2.9 nM。
  • HY-P1868A
    α2β1 Integrin Ligand Peptide TFA 99.33%
    α2β1 Integrin Ligand Peptide TFA 在细胞膜表面与 α2β1 整合素受体相互作用,进入细胞介导细胞外信号。α2β1 Integrin Ligand Peptide是一种潜在的胶原受体拮抗剂。
  • HY-130119
    Integrin-IN-2 Inhibitor
    Integrin-IN-2 是口服生物利用泛 αv 整联蛋白 (αv integrin) 抑制剂。Integrin-IN-2 可以增加 αvβ6αvβ3αvβ5αvβ8 的结合亲和力,pIC50 值分别为 7.8、8.4、8.4 和 7.4。
  • HY-14951
    Firategrast Antagonist 99.66%
    Firategrast 是一种口服 α4β1/α4β7 整合素拮抗剂。
  • HY-100506
    GLPG0187 Antagonist 98.97%
    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-N0416
    Cucurbitacin B Inhibitor 99.92%
    葫芦素B (Cucurbitacin B)是一具有抗癌活性的天然化合物。
  • HY-12290
    Arg-Gly-Asp-Ser Inhibitor >98.0%
  • HY-14571
    E7820 Inhibitor 99.36%
    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-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-15770
    TR-14035 Antagonist
    TR-14035是α4β7/α4β1 integrin拮抗剂,IC50为7 nM和87 nM。
  • HY-17369
    Tirofiban hydrochloride monohydrate Antagonist 99.99%
  • HY-B0686
    Eptifibatide Inhibitor
    Eptifibatide 是一种环状七肽,为 glycoprotein IIb/IIIa 受体抑制剂,具有抗血小板活性。
  • HY-19344
    Lifitegrast Antagonist 99.58%
    Lifitegrast (SAR 1118) 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-15102
    MK-0429 Antagonist 99.73%
    MK-0429 (L-000845704) 是可口服,高效,选择性,非多肽αvβ3 整合素拮抗剂,IC50为80 nM。
  • HY-70073
    Zaurategrast Inhibitor 98.81%
    Zaurategrast (CT7758) 是一种口服有效的 α4-integrin 抑制剂。
Isoform Specific Products

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