1. Signaling Pathways
  2. Cytoskeleton
  3. Integrin

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 (43):

Cat. No. Product Name Effect Purity
  • HY-16141
    Cilengitide Inhibitor 99.06%
    Cilengitide is a potent and selective integrin inhibitor for αvβ3 and αvβ5 receptor, with IC50s of 4 and 79 nM, respectively.
  • HY-P0023
    Cyclo(-RGDfK) Inhibitor >98.0%
    Cyclo(-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM.
  • HY-18644
    CWHM-12 Inhibitor 99.65%
    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-18676
    OSU-T315 Inhibitor 99.88%
    OSU-T315 (ILK-IN-1) is a small Integrin-linked kinase (ILK) inhibitor with an IC50 of 0.6 μM, inhibiting PI3K/AKT signaling by dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain). OSU-T315 abrogates AKT activation by impeding AKT localization in lipid rafts and triggers caspase-dependent apoptosis in an ILK-independent manner. OSU-T315 causes cell death through apoptosis and autophagy.
  • HY-12290
    Arg-Gly-Asp-Ser Inhibitor >98.0%
    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-P9911
    Vedolizumab Antagonist 99.64%
    Vedolizumab is a humanized monoclonal antibody that targets the α4β7 integrin for the treatment of ulcerative colitis and Crohn's disease.
  • HY-P1740A
    RGD peptide (GRGDNP) TFA Inhibitor 98.80%
    RGD peptide (GRGDNP) (TFA) acts as an inhibitor of integrin-ligand interactions and plays an important role in cell adhesion, migration, growth, and differentiation. RGD peptide (GRGDNP) (TFA) promote apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing.
  • HY-111413
    c(phg-isoD-G-R-(NMe)k) Inhibitor
    c(phg-isoD-G-R-(NMe)k) is a selective α5β1 integrin ligand with an IC50 of 2.9 nM.
  • HY-100506
    GLPG0187 Antagonist 98.97%
    GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits αvβ1-integrin with an IC50 of 1.3 nM.
  • HY-14571
    E7820 Inhibitor 99.36%
    E7820 is an angiogenesis inhibitor by suppressing integrin a2, a cell adhesion molecule expressed on endothelial cells.
  • HY-14951
    Firategrast Antagonist 99.66%
    Firategrast is an orally bioavailable α4β1/α4β7 integrin antagonist.
  • HY-17369
    Tirofiban hydrochloride monohydrate Antagonist 99.99%
    Tirofiban hydrochloride monohydrate is a potent non-peptide, glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) antagonist IC50 value: Target: integrin IIb/IIIa Tirofiban hydrochloride monohydrate blocks platelet aggregation and thrombus formation.
  • HY-N0416
    Cucurbitacin B Inhibitor 99.92%
    Cucurbitacin B belongs to a class of highly oxidized tetracyclic triterpenoids; could repress cancer cell progression.
  • HY-P0122
    iRGD peptide 98.62%
    iRGD peptide is a 9-amino acid cyclic peptide, triggers tissue penetration of drugs by first binding to av integrins, then proteolytically cleaved in the tumor to produce CRGDK/R to interact with neuropilin-1, and has tumor-targeting and tumor-penetrating properties.
  • HY-B0686
    Eptifibatide Inhibitor
    Eptifibatide is a cyclic heptapeptide, acts as a competitive antagonist for the activated platelet glycoprotein IIb/IIIa receptor, with anti-platelet activity.
  • 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-15770
    TR-14035 Antagonist
    TR-14035 is a a dual alpha4beta7(IC50=7 nM)/alpha4beta1 (IC50=87 nM) integrin antagonist .
  • HY-19344
    Lifitegrast Antagonist 99.12%
    Lifitegrast (SAR 1118) 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-70073
    Zaurategrast Inhibitor 98.81%
    Zaurategrast (CT7758) is a potent and oral-effective α4-integrin inhibitor.
  • HY-P0278A
    RGD Trifluoroacetate >98.0%
    RGD Trifluoroacetate is a tripeptide that effectively triggers cell adhesion, addresses certain cell lines and elicits specific cell responses; RGD Trifluoroacetate binds to integrins.
Isoform Specific Products

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