1. Signaling Pathways
  2. Cytoskeleton
  3. Integrin

Integrin (整合素)

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 Isoform Specific Products:

  • αvβ1

  • αvβ3

  • αvβ5

  • αvβ6

  • αvβ8

  • α5β1

  • α1β1

  • α4β1

  • α6β1

  • α9β1

  • αIIbβ3

  • α4β7

  • αLβ2

Integrin 相关产品 (52):

Cat. No. Product Name Effect Purity
  • HY-16141
    Cilengitide Inhibitor 99.32%
    Cilengitide (EMD 121974) 是一种有效的选择性整合素 ανβ3ανβ5 抑制剂。Cilengitide 抑制 ανβ3 和 ανβ5 与玻连蛋白结合,IC50 值分别为 4 和 79 nM。
  • HY-P0122
    iRGD peptide 99.03%
    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-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-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-15102
    MK-0429 Antagonist 99.84%
    MK-0429 (L-000845704) 是可口服,高效,选择性,非多肽整合素泛拮抗剂,对αvβ1、αvβ3、αvβ5、αvβ6、αvβ8 和 α5β1 的 IC5 0 值分别为1.6 nM、2.8 nM、0.1 nM、0.7 nM、0.5 nM 和 12.2 nM。
  • HY-14571
    E7820 Inhibitor 99.36%
    E7820 (ER68203-00) 是一种具有口服活性芳香族磺酰胺衍生物,是一种独特的血管生成 (angiogenesis) 抑制剂,可抑制内皮上整合素 α2 (integrin alpha2) 亚基的表达。E7820 抑制大鼠主动脉血管生成,IC50 为 0.11 μg/ml。E7820 调节 α-1,α-2,α-3 和 α-5 整联素 mRNA 表达。具有抗血管生成和抗肿瘤活性。
  • 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-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-12290
    Arg-Gly-Asp-Ser Inhibitor >98.0%
    Arg-Gly-Asp-Ser是整联蛋白结合序列,抑制整联蛋白受体功能,通过抑制胶原蛋白引发的白细胞活化减少全身炎症,并减弱炎性细胞因子,iNOS和MMP-9的表达。
  • 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-B0686
    Eptifibatide Inhibitor 99.91%
    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-15770
    TR-14035 Antagonist
    TR-14035 是一种 α4β74β1 整合素双重抑制剂,对 α4β7 和 α4β1 作用的 IC50 值分别为 7 nM和 87 nM。TR-14035 可用于炎症和自体免疫疾病的研究。
  • HY-100563
    Cyclo(RGDyK) trifluoroacetate Inhibitor 99.13%
    Cyclo(RGDyK) trifluoroacetate 是一种有效的选择性 αVβ3 整联蛋白 (integrin) 抑制剂,IC50 为 20 nM。
  • HY-100226
    A-205804 Inhibitor 98.12%
    A-205804 是抑制 E-selectinICAM-1 表达的口服有效的,高效、选择性的先导抑制剂,对 E-selectin 和 ICAM-1 作用的 IC50 分别为 20 nM 和 25 nM。A-205804 可用于慢性炎症疾病的研究。
  • HY-17369
    Tirofiban hydrochloride monohydrate Antagonist >98.0%
    Tirofiban盐酸盐一水合物是非肽类,糖蛋白IIb/IIIa拮抗剂。
  • HY-U00003
    ICAM-1-IN-1 Inhibitor 99.96%
    ICAM-1-IN-1 是有效,选择性的 E-selectinICAM-1 抑制剂,IC50值分别为7和5 nM。
  • HY-P0290A
    GRGDSP TFA Inhibitor 98.53%
    GRGDSP (TFA) 是一种整联蛋白 (integrin) 抑制剂。
  • HY-P1740A
    RGD peptide (GRGDNP) (TFA) Inhibitor 98.80%
    RGD peptide (GRGDNP) (TFA)作为整合素-配体相互作用的抑制剂,在细胞黏附、迁移、生长和分化中发挥重要作用。RGD peptide (GRGDNP) (TFA)通过激活构象变化促进细胞凋亡,从而增强caspase-3的活化。
  • 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-P9911
    Vedolizumab Antagonist 99.64%
    Vedolizumab是一种靶向α4β7整联蛋白 (integrin) 的人源化单克隆抗体,用于溃疡性结肠炎和克罗恩病的相关研究。
Isoform Specific Products

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