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-100445
    αvβ1 integrin-IN-1
    Inhibitor 99.51%
    αvβ1 integrin-IN-1 (Compound C8) is a potent and selective αvβ1 integrin inhibitor with an IC50 of 0.63 nM. Antifibrotic effects.
    αvβ1 integrin-IN-1
  • HY-P0295
    Gly-Arg-Gly-Asp-Ser
    Inhibitor 99.91%
    Gly-Arg-Gly-Asp-Ser (GRGDS) is a pentapeptide that forms the cell-binding domain of a glycoprotein, osteopontin. Gly-Arg-Gly-Asp-Ser binds to integrin receptors αvβ3 and αvβ5 with estimated IC50 of ~5 and ~6.5 μM
    Gly-Arg-Gly-Asp-Ser
  • HY-139702
    α5β1 integrin agonist-1
    Agonist 99.52%
    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.
    α5β1 integrin agonist-1
  • HY-164957
    SGN-B6A
    Inhibitor 99.68%
    SGN-B6A is an ADC, which targets integrin beta-6 (ITGB6) through human IgG1 monoclonal antibody Sigvotatug (HY-P990764), and exhibits cytotoxicity against multiple integrin beta-6-positive cancer cell through mitotic inhibitor MMAE (HY-15162).
    SGN-B6A
  • HY-120628
    BMS-587101
    Antagonist 99.39%
    BMS-587101 is a potent and orally active antagonist of leukocyte function associated antigen-1 (LFA-1). BMS-587101 has anti-inflammatory effects and can be used for rheumatoid arthritis research.
    BMS-587101
  • HY-P99291
    Etaracizumab
    Inhibitor ≥99.0%
    Etaracizumab (LM 609) is an αvβ3 integrin IgG mAb. Etaracizumab is developed to target αvβ3+ cancer cells via NK cell-mediated cytotoxicity. Etaracizumab sterically hinders access of large ligands to the RGD-binding pocket, without obstructing it. Etaracizumab decreases p-Akt in vitro. Etaracizumab can decrease cancer proliferation and invasion. Etaracizumab induces tumor cell apoptosis, and inhibition ofαvβ3-mediated cell adhesion, endothelial cell migration and osteoclast-mediated bone resorption. Etaracizumab can be studied in anti-tumor research against cancers such as ovarian cancer, metastatic melanoma as well as advanced solid tumors. Recommend Isotype Control: Human IgG1 kappa, Isotype Control (HY-P99001).
    Etaracizumab
  • HY-N2584A
    Isoxanthohumol
    Inhibitor 99.91%
    Isoxanthohumol is an orally active flavonoid compound. Isoxanthohumol has biological activities such as anti-tumor, anti-inflammatory, antioxidant, antiviral, antifungal, and inhibition of adipogenesis. Isoxanthohumol can induce apoptosis, autophagy, and migration of tumor cells. Isoxanthohumol is active against viruses such as HSV, BVDV, CMV, and Rhino. Isoxanthohumol can be used for the research of tumors, metabolic, and inflammatory diseases.
    Isoxanthohumol
  • HY-145728B
    (R/S)-Alicaforsen
    Inhibitor
    (R/S)-Alicaforsen is the racemate of Alicaforsen composed of R and S configurations. Alicaforsen 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.
    (R/S)-Alicaforsen
  • HY-W588250
    Surfactin C1
    Antagonist 99.36%
    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.
    Surfactin C1
  • HY-101473
    EMD527040
    Inhibitor 99.94%
    EMD527040 is a potent and highly selective αvβ6 antagonist with antifibrotic activities. EMD527040 can be used for carcinoma and liver fibrosis research.
    EMD527040
  • HY-P0178A
    LXW7 TFA
    Inhibitor 98.44%
    LXW7 TFA, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC50 of 0.68 μM. LXW7 TFA increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect.
    LXW7 TFA
  • HY-P0031
    Cyclo(RADfK)
    Modulator
    Cyclo(RADfK) can be used as a control for Cyclo(-RGDfK) (HY-P0023).
    Cyclo(RADfK)
  • HY-19767
    GSK 3008348
    99.27%
    GSK 3008348 is a small molecule integrin αvβ6 antagonist, extracted from patent WO/2014154725A1, example 1. The affinity (pIC50) for the human - a 6 protein in the Fluorescence Polarisation Assay for Integrin Antagonist 1 was 8.1, whereas its affinity in the cell Adhesion Assays was for: ανβ6 (pIC50 = 8.4); ανβ3 (pIC50 = 6); ανβ5 (pIC50 = 6.9); ανβ8 (pIC50 = 7.7).
    GSK 3008348
  • HY-14126
    BIO-1211
    Inhibitor 99.81%
    BIO-1211 is a highly selective and orally active α4β1 (VLA-4) inhibitor, with IC50 values of 4 nM and 2 μM for α4β1 and α4β7, respectively.
    BIO-1211
  • HY-P1189A
    Echistatin TFA
    Antagonist 98.05%
    Echistatin TFA, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1.
    Echistatin TFA
  • HY-P1613A
    Cyclo(Arg-Gly-Asp-D-Phe-Val) TFA
    Inhibitor 99.77%
    Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) (Cyclo(RGDfV) (TFA))is an integrin αvβ3 inhibitor. Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) has antitumor activity. Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) can be used for the research of acute myeloid leukemia.
    Cyclo(Arg-Gly-Asp-D-Phe-Val) TFA
  • HY-P0309A
    Arg-Gly-Glu-Ser TFA
    Control 99.39%
    Arg-Gly-Glu-Ser TFA is a polypeptide related to RGD and is a negative control for Arg-Gly-Asp-Ser (HY-12290).
    Arg-Gly-Glu-Ser TFA
  • HY-P2532
    Integrin Binding Peptide
    99.73%
    Integrin Binding Peptide is derived by fibronectin. Integrin Binding Peptide can be used for PEG hydrogel preparation.
    Integrin Binding Peptide
  • HY-P99473
    Bersanlimab
    Inhibitor 99.77%
    Bersanlimab (BI-505) is a fully human monoclonal antibody that targets intercellular adhesion molecule-1 (ICAM-1 or CD54). Bersanlimab has anticancer effects.
    Bersanlimab
  • HY-P1187
    HSDVHK-NH2
    Antagonist 99.28%
    HSDVHK-NH2 is an antagonist of the integrin αvβ3-vitronectin interaction, with an IC50 of 1.74 pg/mL (2.414 pM).
    HSDVHK-NH2
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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