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  3. Integrin

Integrin

Integrin

Related Products

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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 (145):

Cat. No. Product Name Effect Purity
  • HY-100506
    GLPG0187 Antagonist 99.78%
    GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits αvβ1-integrin with an IC50 of 1.3 nM[1]. GLPG0187 inhibits migrasome biogenesis without cytotoxicity[3].
  • HY-16141
    Cilengitide Antagonist 99.36%
    Cilengitide (EMD 121974) is a potent integrins antagonist with IC50s of 0.61 nM (ανβ3), 8.4 nM (ανβ5) and 14.9 nM (α5β1), respectively. Cilengitide inhibits the binding of ανβ3 and ανβ5 to Vitronectin with IC50s of 4 nM and 79 nM, respectively. Cilengitide inhibits TGF-β/Smad signaling, mediates PD-L1 expression. Cilengitide also induces apoptosis, shows antiangiogenic effect in the research against glioblastoma and other cancers[1][2][3].
  • 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-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-W588250
    Surfactin C1 Antagonist
    Surfactin C1 is an amphiphilic biosurfactants. Surfactin C1 inhibits leukemic cell (HL-60) adhesion to human umbilical vein endothelial cells (HUVEC). Surfactin C1 inhibits adhesion melecules expression, such as ICAM-1 and VCAM-1[1].
  • HY-P99891
    Rovelizumab Inhibitor
    Rovelizumab is a humanized monoclonal leukointegrin antibody. Rovelizumab is a monoclonal antibody directed against the CD11/CD18 cell adhesion proteins. Rovelizumab can be used for research of multiple sclerosis (MS), hemorrhagic shock, myocardial infarction (MI) and stroke[1].
  • HY-P99765
    Odulimomab Inhibitor
    Odulimomab (anti-LFA1) is an anti-LFA-1 monoclonal antibody. Odulimomab inhibits proliferation of T lymphocyte and shows protective effects against ischemia and reperfusion injury. Odulimomab can be used for the research of transplant rejection and immunological disease[1][2].
  • HY-P3160
    Fibronectin Modulator
    Fibronectin, a glycoprotein (~500 kDa) present in blood as well as in cells, is a biomarker of tissue injury. Fibronectin binds to membrane-spanning receptor proteins called integrins. Fibronectin also binds to other extracellular matrix proteins such as collagen, fibrin, and heparan sulfate proteoglycans[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-130119
    Integrin-IN-2 Inhibitor
    Integrin-IN-2 (compound 39) is an orally bioavailable pan αv integrin inhibitor. Integrin-IN-2 can increases the αvβ6, αvβ3, αvβ5 and αvβ8 binding affinities with pIC50 values of 7.8, 8.4, 8.4 and 7.4, respectively[1].
  • HY-N0416
    Cucurbitacin B Inhibitor 99.91%
    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-P1613
    Cyclo(Arg-Gly-Asp-D-Phe-Val) Inhibitor
    Cyclo(Arg-Gly-Asp-D-Phe-Val) is an integrin αvβ3 inhibitor. Cyclo(Arg-Gly-Asp-D-Phe-Val) has antitumor activity. Cyclo(Arg-Gly-Asp-D-Phe-Val) can be used for the research of acute myeloid leukemia[1].
  • HY-P3523
    KGDS Activator
    KGDS is synthetic peptides, targeting integrin GPIIb-IIIa located on the membrane of human activated platelets. Amino acid sequence: Lys-Gly-Asp-Ser[1].
  • HY-19306
    SB-267268 Antagonist
    SB-267268 is a selective and nonpeptidic alpha(v)beta3 (αvβ3) and alpha(v)beta5 (αvβ5) integrins antagonist, with Kis of 0.9, 0.5 and 0.7 nM for human αvβ3, monkey αvβ3 and human αvβ5, respectively. SB-267268 inhibits human and mouse αvβ3 with IC50s of 0.68 and 0.29 nM, respectively. SB-267268 reduces angiogenesis and VEGF expression[1].
  • HY-P1740
    RGD peptide (GRGDNP) Inhibitor
    RGD peptide (GRGDNP) is an inhibitor of integrin-ligand interactions. RGD peptide (GRGDNP) competitively inhibits α5β1 binding with extracellular matrice (ECM). RGD peptide (GRGDNP) promotes apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing. RGD peptide (GRGDNP) plays an important role in cell adhesion, migration, growth, and differentiation[1][2][3].
  • HY-47888
    PLN-1474 Inhibitor 99.30%
    PLN-1474 (compound 1) is an orally active and selective avß1 integrin inhibitor with an IC50 value of ＜50 nM. PLN-1474 reduces levels of pSMAD3/SMAD3 in liver, hepatic collagen gene expression and hepatic OHP concentration in liver fibrosis mouse model. PLN-1474 can be used for the research of preventing, delaying or treating a fibrotic or cirrhotic disease or disorder[1].
  • HY-P1868A
    α2β1 Integrin Ligand Peptide TFA 98.80%
    α2β1 Integrin Ligand Peptide TFA interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors[1].
  • HY-N10438
    Ganodermaones B Inhibitor
    Ganodermaones B (Compound 2) is a renal fibrosis inhibitor. Ganodermaones B inhibits TGF-β1-induced collagen I and fibronectin expression[1].