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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 (36):

Cat. No.Product NameEffectPurity
  • HY-16141
    CilengitideInhibitor 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-18644
    CWHM-12Inhibitor 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-12290
    Arg-Gly-Asp-SerInhibitor >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-18676
    OSU-T315Inhibitor 99.42%
    OSU-T315是整联蛋白连接激酶 (ILK) 的抑制剂,IC50 为600 nM。
  • HY-100563
    Cyclo(RGDyK) trifluoroacetateInhibitor 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-75385
    Zaurategrast ethyl esterAntagonist 99.06%
    Zaurategrast ethyl ester (CDP323) 是 CT7758 的乙酯前药,是 α4β1/α4β7 整联蛋白拮抗剂,可用于治疗炎症和自身免疫疾病。
  • HY-P0290A
    GRGDSP TFAInhibitor 98.53%
    GRGDSP (TFA) 是一种整联蛋白 (integrin) 抑制剂。
  • HY-14571
    E7820Inhibitor 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
    GLPG0187Antagonist 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-13535A
    ATN-161 trifluoroacetate saltAntagonist
    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-14951
    FirategrastAntagonist 99.66%
    Firategrast 是一种口服 α4β1/α4β7 整合素拮抗剂。
  • HY-N0416
    Cucurbitacin BInhibitor 99.92%
    葫芦素B (Cucurbitacin B)是一具有抗癌活性的天然化合物。
  • HY-17369
    Tirofiban hydrochloride monohydrateAntagonist 99.99%
    Tirofiban盐酸盐一水合物是非肽类,糖蛋白IIb/IIIa拮抗剂。
  • 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-B0686
    EptifibatideInhibitor
    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
    LifitegrastAntagonist 99.12%
    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-70073
    ZaurategrastInhibitor 98.81%
    Zaurategrast (CT7758) 是一种口服有效的 α4-integrin 抑制剂。
  • HY-15770
    TR-14035Antagonist
    TR-14035是α4β7/α4β1 integrin拮抗剂,IC50为7 nM和87 nM。
  • 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。
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