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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 (88):

Cat. No. Product Name Effect Purity
  • HY-16141
    Cilengitide Inhibitor 99.32%
    Cilengitide (EMD 121974) is a potent and selective inhibitor of the integrins ανβ3 and ανβ5. Cilengitide inhibits binding of isolated ανβ3 and ανβ5 to Vitronectin with an IC50 value of 4 and 79 nM, respectively [1].
  • 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-15102
    MK-0429 Antagonist 99.84%
    MK-0429 (L-000845704) is an orally active, potent, selective and nonpeptide pan-integrin antagonist with IC50 values of 1.6 nM, 2.8 nM, 0.1 nM, 0.7 nM, 0.5 nM and 12.2 nM for αvβ1, αvβ3, αvβ5, αvβ6, αvβ8 and α5β1, respectively[1][2][3].
  • HY-P0023
    Cyclo(-RGDfK) Inhibitor
    Cyclo(-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM[1]. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface[2].
  • HY-14571
    E7820 Inhibitor 99.25%
    E7820 (ER68203-00), an orally active aromatic sulfonamide derivative, is a unique angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium. E7820 inhibits rat aorta angiogenesis with an IC50 of 0.11 μg/ml. E7820 modulates α-1, α-2, α-3, and α-5 integrin mRNA expression. Antiangiogenic and antitumor activity[1][2].
  • HY-139702
    α5β1 integrin agonist-1 Agonist
    α5β1 integrin agonist-1, acting as α5β1 integrin agonist, is able to selectively deliver 5-FU into tumor cells, successfully leading to cancer cell death.
  • HY-139202
    XVA143 Inhibitor
    XVA143, an α/β I-like allosteric antagonist, inhibits LFA-1 dependent firm adhesion, while at the same time it enhances adhesion in shear flow and rolling both in vitro and in vivo[1].
  • HY-107587
    A-286982 Inhibitor 99.69%
    A-286982 is a potent and allosteric LFA-1/ICAM-1 interaction inhibitor with IC50s of 44 nM and 35 nM in an LFA-1/ICAM-1 binding and LFA-1-mediated cellular adhesion assay, respectively[1][2].
  • HY-P0122
    iRGD peptide 99.03%
    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-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-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-19344
    Lifitegrast Antagonist 99.58%
    Lifitegrast (SAR 1118) is an integrin lymphocyte function-associated antigen-1 (LFA-1; αLβ2) antagonist; inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM[1].
  • HY-N0416
    Cucurbitacin B Inhibitor 99.92%
    Cucurbitacin B belongs to a class of highly oxidized tetracyclic triterpenoids; could repress cancer cell progression.
  • HY-12290
    Arg-Gly-Asp-Ser Inhibitor
    Arg-Gly-Asp-Ser is an integrin binding sequence that inhibits integrin receptor function. Arg-Gly-Asp-Ser directly and specifically bind pro-caspase-8, pro-caspase-9 and pro-caspase-3, while it does not bind pro-caspase-1.
  • HY-100226
    A-205804 Inhibitor 98.12%
    A-205804 is an orally bioavailable, potent and selective lead inhibitor of E-selectin and ICAM-1 expression, with an IC50 of 20 nM and 25 nM for E-selectin and ICAM-1, respectively. A-205804 can be used in the research of chronic inflammatory diseases[1].
  • HY-P0278A
    RGD Trifluoroacetate
    RGD Trifluoroacetate is a tripeptide that effectively triggers cell adhesion, addresses certain cell lines and elicits specific cell responses; RGD Trifluoroacetate binds to integrins.
  • HY-100445A
    αvβ1 integrin-IN-1 TFA Inhibitor 98.30%
    αvβ1 integrin-IN-1 TFA (Compound C8) is a potent and selective αvβ1 integrin inhibitor with an IC50 of 0.63 nM. Antifibrotic effects[1].
  • HY-115677
    ILK-IN-3 Inhibitor 99.57%
    ILK-IN-3 is an integrin linked kinase inhibitor with antitumor activity[1].
  • HY-14951
    Firategrast Antagonist 99.88%
    Firategrast (SB 683699) is an orally active and specific α4β1/α4β7 integrin antagonist. Firategrast reduces trafficking of lymphocytes into the central nervous system (CNS) and decreases multiple sclerosis (MS) activity[1][2][3].
  • HY-15701
    Leukadherin-1 Agonist
    Leukadherin-1, a specific agonist of the leukocyte surface integrin CD11b/CD18, increases CD11b/CD18-dependent cell adhesion to fibrinogen with an EC50 of 4 μM. Leukadherin-1 enhances leukocyte adhesion to ligands (such as ICAM-1) and vascular endothelium and thus reduces leukocyte transendothelial migration and influx to the injury sites. Leukadherin-1 suppresses innate inflammatory signaling[1][2][3].