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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 (32):

Cat. No. Product Name Effect Purity
  • HY-16141
    Cilengitide Inhibitor 98.99%
    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-12290
    Arg-Gly-Asp-Ser Inhibitor >98.0%
  • HY-18644
    CWHM-12 Inhibitor 99.65%
    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-18676
    OSU-T315 Inhibitor 99.42%
    OSU-T315是整联蛋白连接激酶 (ILK) 的抑制剂,IC50 为600 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-P0290A
    GRGDSP TFA Inhibitor
    GRGDSP (TFA) 是一种整联蛋白 (integrin) 抑制剂。
  • HY-P1613A
    Cyclo(Arg-Gly-Asp-D-Phe-Val) TFA Inhibitor 99.40%
    Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) 是整合蛋白 αvβ3 的抑制剂,具有抗肿瘤活性。
  • HY-14571
    E7820 Inhibitor 98.62%
    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-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-14951
    Firategrast Antagonist 99.66%
    Firategrast 是一种口服 α4β1/α4β7 整合素拮抗剂。
  • 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-17369
    Tirofiban hydrochloride monohydrate Antagonist 99.99%
  • HY-N0416
    Cucurbitacin B Inhibitor 99.68%
    葫芦素B (Cucurbitacin B)是一具有抗癌活性的天然化合物。
  • HY-B0686
    Eptifibatide Inhibitor
  • 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-70073
    Zaurategrast Inhibitor 98.81%
    Zaurategrast 是一种口服有效的 α4-integrin 抑制剂。
  • 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-P0278A
    RGD Trifluoroacetate >98.0%
    RGD Trifluoroacetate 是一种三肽,能够有效的引起细胞黏着,定位某种特定细胞系并产生特定的细胞反应;RGD Trifluoroacetate 能够与 integrins 结合。
  • HY-P0031
    Cyclo(RADfK) Modulator
    Cyclo(RADfK) 是选择性 α(v)β(3) 整合素配体, 广泛用于新血管生成的研究, 治疗和诊断。
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