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 Isoform Specific Products:

  • αvβ1

  • αvβ3

  • αvβ5

  • αvβ6

  • αvβ8

  • α5β1

  • α2β1

  • α4β1

  • α9β1

  • αIIbβ3

  • α4β7

  • αLβ2

Integrin Related Products (87):

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 .
  • 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.
  • 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. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface.
  • 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-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.
  • HY-138542
    RO0270608
    Antagonist
    RO0270608, the active metabolite of R411, is a dual alpha4beta1-alpha4beta7 (α4β1/α4β7) integrin antagonist. Antiinflammatory activity.
  • HY-101473
    EMD527040
    Inhibitor
    EMD527040 is a potent and highly selective αvβ6 antagonist with antifibrotic activities. EMD527040 can be used for carcinoma and liver fibrosis research.
  • 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.
  • 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.
  • 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 ≥98.0%
    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-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.
  • 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.
  • 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.
  • 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.
  • HY-18676
    OSU-T315
    Inhibitor ≥98.0%
    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-115677
    ILK-IN-3
    Inhibitor 99.57%
    ILK-IN-3 is an integrin linked kinase inhibitor with antitumor activity.
Isoform Specific Products

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