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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 Related Products (19):

Cat. No. Product Name Effect Purity
  • HY-16141
    Cilengitide Inhibitor
    Cilengitide is a potent and selective integrin inhibitor for αvβ3 and αvβ5 receptor, inhibits binding of isolated αvβ3 and αvβ5 to vitronectin with an IC50 value of 4 and 79 nM, respectively.
  • HY-18644
    CWHM-12 Inhibitor
    CWHM-12 is a potent inhibitor of αV integrins with IC50s of 0.2, 0.8, 1.5, and 1.8 nM for αvβ8, αvβ3, αvβ6, and αvβ1.
  • HY-12290
    Arg-Gly-Asp-Ser Inhibitor
    Arg-Gly-Asp-Ser is an integrin binding sequence that inhibits integrin receptor function, decreases systemic inflammation via inhibition of collagen-triggered activation of leukocytes and attenuates expression of inflammatory cytokines, iNOS and MMP-9.
  • HY-13535A
    ATN-161 trifluoroacetate salt Antagonist
    ATN-161 trifluoroacetate salt is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.
  • HY-P0023
    Cyclo(-RGDfK) Inhibitor
    Cyclo(-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin.
  • HY-19344
    Lifitegrast Antagonist
    Lifitegrast is an integrin lymphocyte function-associated antigen-1 (LFA-1) antagonist; inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM.
  • HY-14571
    E7820 Inhibitor
    E7820 is an angiogenesis inhibitor by suppressing integrin a2, a cell adhesion molecule expressed on endothelial cells.
  • HY-14951
    Firategrast Antagonist
    Firategrast is an orally bioavailable α4β1/α4β7 integrin antagonist.
  • HY-19767A
    Integrin Antagonist 1 hydrochloride Antagonist
    Integrin Antagonist 1 hydrochloride is a small molecule integrin (alpha)v(beta)6 antagonist, extracted from patent WO/2014154725A1, example 1.
  • HY-70073
    Zaurategrast Inhibitor
    Zaurategrast is a potent and oral-effective α4-integrin inhibitor.
  • HY-18676
    ILK-IN-1 Inhibitor
    ILK-IN-1 is a novel ILK inhibitor with IC50 of 0.6 (mu)M.
  • HY-17369
    Tirofiban hydrochloride monohydrate Antagonist
    Tirofiban hydrochloride monohydrate is a potent non-peptide, glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) antagonist.
  • HY-13535
    ATN-161 Antagonist
    ATN-161 (Ac-PHSCN-NH2) is a five -amino-acid peptide derived from the synergy region of fibronectin; a beta integrin antagonist with antitumor activity.
  • HY-15770
    TR-14035 Antagonist
    TR-14035 is a a dual alpha4beta7(IC50=7 nM)/alpha4beta1 (IC50=87 nM) integrin antagonist .
  • HY-18668
    Integrin Antagonists 27 Antagonist
    Integrin Antagonists 27 is a small molecule integrin (alpha)v(beta)3 antagonist with binding affinity of 18 nM, as s novel anticancer agent.
  • HY-P0031
    Cyclo(RADfK) Modulator
    Cyclo(RADfK) is a selective α(v)β(3) integrin ligand that has been extensively used for research, therapy, and diagnosis of neoangiogenesis.
  • HY-18676B
    ILK-IN-2 Inhibitor
    ILK-IN-2 is a ILK inhibitor.
  • HY-N0416
    Cucurbitacin B Inhibitor
    Cucurbitacin B belongs to a class of highly oxidized tetracyclic triterpenoids; could repress cancer cell progression.
  • HY-17369B
    Tirofiban Antagonist
    Tirofiban(L700462;MK383) is a potent non-peptide, glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) antagonist.