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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 Related Products (30):

Cat. No. Product Name Effect Purity
  • HY-16141
    Cilengitide Inhibitor 98.99%
    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. Sequence: Cyclo(Arg-Gly-Asp-Phe-Lys).
  • 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-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 99.42%
    OSU-T315 is an inhibitor of integrin-linked kinase (ILK) with an IC50 of 600 nM.
  • HY-P1613A
    Cyclo(Arg-Gly-Asp-D-Phe-Val) TFA Inhibitor 99.40%
    Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) is an inhibitor of integrin αvβ3, with antitumor activity.
  • HY-P0290A
    GRGDSP TFA Inhibitor
    GRGDSP (TFA) is an integrin inhibitor.
  • HY-100563
    Cyclo(RGDyK) trifluoroacetate Inhibitor 99.13%
    Cyclo(RGDyK) trifluoroacetate is a potent and selective αVβ3 integrin inhibitor with an IC50 of 20 nM.
  • HY-100506
    GLPG0187 Antagonist 98.08%
    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 98.62%
    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-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-N0416
    Cucurbitacin B Inhibitor 99.68%
    Cucurbitacin B belongs to a class of highly oxidized tetracyclic triterpenoids; could repress cancer cell progression.
  • HY-B0686
    Eptifibatide Inhibitor
    Eptifibatide is an antiplatelet drug of the glycoprotein IIb/IIIa inhibitor class.
  • HY-19344
    Lifitegrast Antagonist 99.12%
    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-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-70073
    Zaurategrast Inhibitor 98.81%
    Zaurategrast 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. Sequence: Arg-Gly-Asp.
  • 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. Sequence: Cyclo(Ala-Asp-Phe-Lys-Arg).
Isoform Specific Products

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