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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P1188
    LDV-FITC
    98.89%
    LDV-FITC, a fluorescent peptide, is a FITC-conjugated LDV peptide (HY-P2267). LDV-FITC binds to the α4β1 integrin with high affinity (Kd: 0.3 nM and 12 nM for binding to U937 cells in the presence and absence of Mn2+ respectively). LDV-FITC can be used to detect α4β1 integrin affinity.
    LDV-FITC
  • HY-124040
    BI-1950
    Inhibitor
    BI-1950 is a highly potent lymphocyte function associated antigen-1 (LFA-1) inhibitor. LFA-1 is an essential component in normal immune system function and a target for agent discovery.
    BI-1950
  • HY-B0932R
    Levocarnitine propionate hydrochloride (Standard)
    Inhibitor
    Adrenalone (hydrochloride) (Standard) is the analytical standard of Adrenalone (hydrochloride). This product is intended for research and analytical applications. Adrenalone hydrochloride is an adrenergic agonist used as a topical vasoconstrictor and hemostatic. Adrenalone hydrochloride is an inhibitor of dopamine β oxidase. Adrenalone hydrochloride is chemically similar to known norepinephrine transporter (NET) ligands with an IC50 of 36.9 μM.
    Levocarnitine propionate hydrochloride (Standard)
  • HY-145728A
    Alicaforsen sodium
    Inhibitor
    Alicaforsen sodium is a 20-base antisense oligonucleotide inhibiting ICAM-1 production, which is an important adhesion molecule involved in leukocyte migration and trafficking to the site of inflammation.
    Alicaforsen sodium
  • HY-19151A
    Fuzapladib sodium
    Inhibitor 99.88%
    Fuzapladib (IS-741) sodium, an orally active leukocyte-function-associated antigen type 1 (LFA-1) activation inhibitor, is a leukocyte adhesion molecule. Fuzapladib sodium is also a phospholipase A2 (PLA2) inhibitor. Fuzapladib sodium exerts anti-inflammatory effects by inhibiting leukocyte migration into the inflammatory site.
    Fuzapladib sodium
  • HY-17369A
    Tirofiban hydrochloride
    Antagonist
    Tirofiban (L700462) hydrochloride is a selective and reversible platelet integrin receptor (Gp IIb/IIIa) antagonist that inhibits fibrinogen binding to this receptor and has antithrombotic activity. Tirofiban hydrochloride induces proliferation and migration on endothelial cell by inducing production of VEGF. Tirofiban hydrochloride can significantly reduces myocardial no-reflow and ischemia-reperfusion injury by alleviating myocardial microvascular structural and endothelial dysfunction in the ischemic area.
    Tirofiban hydrochloride
  • HY-119350C
    Zalunfiban acetate
    Antagonist
    Zalunfiban (RUC-4) acetate is a potent, selective platelet αIIbβ3antagonist (IC50=45 nM). Zalunfiban acetate can be used for the research of myocardial infarction (MI).
    Zalunfiban acetate
  • HY-P5929
    VnP-16
    VnP-16 can promote bone formation by accelerating osteoblast differentiation and activity through direct interaction with β1 integrin followed by FAK activation.
    VnP-16
  • HY-102073
    TG53
    Inhibitor
    TG53 is a potent inhibitor of tissue transglutaminase (TG2) and fibronectin (FN) protein-protein interaction. TG53 inhibits formation of a complex with integrin β1 and activation of FAK and c-Src during SKOV3 cell attachment onto FN. TG53 can be used for ovarian cancer research.
    TG53
  • HY-130060
    12(S)-HETrE
    Inhibitor
    12(S)-HETrE is a fatty acid metabolite that inhibits platelet aggregation. 12(S)-HETrE can be used in thrombosis-related research.
    12(S)-HETrE
  • HY-P1613
    Cyclo(Arg-Gly-Asp-D-Phe-Val)
    Inhibitor
    Cyclo(Arg-Gly-Asp-D-Phe-Val) (Cyclo(RGDfV)) 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.
    Cyclo(Arg-Gly-Asp-D-Phe-Val)
  • HY-172495
    DSPE-PEG3000-iRGD
    DSPE-PEG3000-iRGD is a PEG compound which composed of DSPE and an αv-integrins targeting peptide (iRGD). iRGD peptide binds to αv-integrins, and then proteolytically cleaved in the tumor to produce CRGDK/R to interact with neuropilin-1, and has tumor-targeting and tumor-penetrating properties. DSPE-PEG3000-iRGD can be used for drug delivery.
    DSPE-PEG3000-iRGD
  • HY-149136
    MORF-627
    Inhibitor
    MORF-627 is a selective, orally active inhibitor for integrin αvβ6 with an IC50 of 9.2 nM measuring by human serum ligand binding assay. MORF-627 inhibits αvβ6-mediated TGF-β1 activation with an IC50 of 2.63 nM, inhibits SMAD2/3 phosphorylation with an IC50 of 8.3 nM. MORF-627 ameliorates the Bleomycin (HY-108345)-induced mouse lung fibrosis.
    MORF-627
  • HY-P991254
    VPI-2690B
    Inhibitor
    VPI-2690B is a human monoclonal antibody (mAb) targeting Integrin aVb3. VPI-2690B inhibits TGF-β signaling. VPI-2690B can be used in Diabetic nephropathies research.
    VPI-2690B
  • HY-137561A
    Bexotegrast hydrochloride
    Inhibitor
    Bexotegrast hydrochloride (PLN-74809 hydrochloride) is a small molecule dual selective inhibitor with activity targeting αVβ1 and αVβ6. Bexotegrast hydrochloride is used for idiopathic pulmonary fibrosis (IPF) and primary sclerosing cholangitis (PSC). Bexotegrast hydrochloride inhibits the activation of TGF-β1 by blocking the function of these integrins, thereby preventing the growth of fibrous tissue in the lungs and bile ducts.
    Bexotegrast hydrochloride
  • 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.
    Ganodermaones B
  • HY-N8903
    Mumefural
    Inhibitor
    Mumefural is a bioactive component of the processed fruit of Prunus mume Sieb. Mumefural inhibits platelet aggregation. Mumefural shows anti-thrombotic effects and ameliorates cognitive impairment.
    Mumefural
  • HY-172493
    DSPE-PEG1000-iRGD
    DSPE-PEG1000-iRGD is a PEG compound which composed of DSPE and an αv-integrins targeting peptide (iRGD). iRGD peptide binds to αv-integrins, and then proteolytically cleaved in the tumor to produce CRGDK/R to interact with neuropilin-1, and has tumor-targeting and tumor-penetrating properties. DSPE-PEG1000-iRGD can be used for drug delivery.
    DSPE-PEG1000-iRGD
  • HY-P10704
    C16Y
    Inhibitor
    C16Y is a short peptide and an inhibitor of integrins αvβ3 and α5β1. C16Y acts on the cell membrane and exerts its anticancer activity by inhibiting angiogenesis .
    C16Y
  • HY-172494
    DSPE-PEG2000-iRGD
    DSPE-PEG2000-iRGD is a PEG compound which composed of DSPE and an αv-integrins targeting peptide (iRGD). iRGD peptide binds to αv-integrins, and then proteolytically cleaved in the tumor to produce CRGDK/R to interact with neuropilin-1, and has tumor-targeting and tumor-penetrating properties. DSPE-PEG2000-iRGD can be used for drug delivery.
    DSPE-PEG2000-iRGD
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