2. Signaling Pathways
  3. Cytoskeleton
  4. Integrin

Integrin

Integrin

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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 Isoform Specific Products:

Integrin Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-13535A
    ATN-161 trifluoroacetate salt
    		Antagonist 99.04%
    ATN-161 trifluoroacetate salt is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.
    ATN-161 trifluoroacetate salt
  • HY-15102
    MK-0429
    		Antagonist 99.50%
    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.
    MK-0429
  • HY-17369B
    Tirofiban
    		Antagonist 99.95%
    Tirofiban (L700462) is a selective and reversible platelet integrin receptor (Gp IIb/IIIa) antagonist that inhibits fibrinogen binding to this receptor and has antithrombotic activity. Tirofiban induces proliferation and migration on endothelial cell by inducing production of VEGF. Tirofiban can significantly reduces myocardial no-reflow and ischemia-reperfusion injury by alleviating myocardial microvascular structural and endothelial dysfunction in the ischemic area.
    Tirofiban
  • HY-107588
    TC-I 15
    		Inhibitor 99.94%
    TC-I 15 (TC-I-15) is a type of allosteric collagen-binding integrin α2β1 inhibitor, and it also inhibits α1β1 and α11β1. TC-I 15 inhibits platelet adhesion to collagen and thrombus deposition. TC-I 15 prevents the formation of a pre-metastatic microenvironment by inhibiting the uptake of cancer-associated fibroblast (CAF) extracellular vesicles (EVs) by lung fibroblasts, which reduces the metastasis of salivary gland adenocystic carcinoma (SACC) to the lungs in mouse models, .
    TC-I 15
  • HY-13535
    ATN-161
    		Antagonist 99.36%
    ATN-161 is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.
    ATN-161
  • HY-B0686
    Eptifibatide
    		Inhibitor 99.79%
    Eptifibatide is a cyclic heptapeptide, acts as a competitive antagonist for the activated platelet glycoprotein IIb/IIIa receptor, with anti-platelet activity.
    Eptifibatide
  • HY-P99227
    Caplacizumab (His Tag)
    		Inhibitor ≥99.0%
    Caplacizumab (His Tag) is a humanized anti-von Willebrand factor (vWF) nanobody. Caplacizumab (His Tag) inhibits the binding of vWF with platelet glycoprotein (GP) Ibα. Caplacizumab (His Tag) inhibits the vWF-mediated platelet adhesion and prevents further microthrombi formation. Caplacizumab (His Tag) can be used for the research of thrombotic thrombocytopenic purpura (TTP).
    Caplacizumab (His Tag)
  • HY-P0290
    GRGDSP
    		Inhibitor 99.95%
    GRGDSP, a synthetic linear RGD peptide, is an integrin inhibitor.
    GRGDSP
  • HY-16143
    Cilengitide TFA
    		Inhibitor 99.92%
    Cilengitide is a potent and selective integrin inhibitor for αvβ3 and αvβ5 receptor, with IC50 values of 4 nM and 79 nM, respectively.
    Cilengitide TFA
  • HY-108831
    Natalizumab
    		Inhibitor 99.10%
    Natalizumab (AN100226; BG00002) is a humanized monoclonal IgG4 antibody inhibitor that selectively targets α4 integrin (CD49d). It blocks the interaction of integrins such as α4β1 (VLA-4) with vascular cell adhesion molecule VCAM-1, intercellular adhesion molecule ICAM-1, and fibronectin by competitively binding to the α4 subunit. Natalizumab inhibits the adhesion, retention, and transendothelial migration of immune cells (such as CD4+ T cells), reducing the infiltration of inflammatory cells into the central nervous system or lesion sites, thus exerting anti-inflammatory and immunomodulatory activity. Natalizumab is used in the study of relapsing-remitting multiple sclerosis (RRMS) and also has applications in the study of autoimmune or inflammation-related diseases such as Crohn's disease, B-cell lymphoma, and non-infectious uveitis. Natalizumab can also prevent lymphocytes from entering the central nervous system, thereby preventing acute demyelinating relapses.
    Natalizumab
  • HY-P0204A
    Endothelin-3, human, mouse, rabbit, rat TFA
    		99.57%
    Endothelin-3, human, mouse, rabbit, rat TFA (Endothelin 3 (Rat,Human) TFA) is an adhesion stimulant. Endothelin-3, human, mouse, rabbit, rat TFA stimulates the adhesion of enteric neural crest cells to various ECM components. Endothelin-3, human, mouse, rabbit, rat TFA plays an important role in the maintenance and self-renewal of intestinal progenitor cells, participates in the migration of enteric neural crest cells, and helps maintain a suitable environment for the colonization of enteric neural crest cells. Endothelin-3, human, mouse, rabbit, rat TFA acts synergistically with the β1-integrin signaling pathway during enteric nervous system development. Endothelin-3, human, mouse, rabbit, rat TFA can be used in studies related to distal aganglionosis.
    Endothelin-3, human, mouse, rabbit, rat TFA
  • HY-P0122
    iRGD peptide
    		98.49%
    iRGD peptide is a 9-amino acid cyclic peptide, triggers tissue penetration of agents by first binding to αv-integrins, then proteolytically cleaved in the tumor to produce CRGDK/R to interact with neuropilin-1, and has tumor-targeting and tumor-penetrating properties.
    iRGD peptide
  • HY-100226
    A-205804
    		Inhibitor 98.96%
    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.
    A-205804
  • HY-P99333
    Volociximab
    		Inhibitor ≥99.0%
    Volociximab (M200) is a chimeric human/murine IgG4 antibody IIA1 targeting integrin α5β1 (EC50=0.2 nM). Integrin α5β1 is a major fibronectin receptor involved in angiogenesis. Volociximab has antiangiogenic and antitumor activities and inhibits the proliferation of human umbilical vein vascular endothelial cells (HUVECs).
    Volociximab
  • HY-110112
    BTT-3033
    		Inhibitor
    BTT-3033 is an orally active conformation-selective inhibitor of α2β1 (EC50: 130 nM) by binding to the α2I domain. BTT-3033 inhibits platelet binding to collagen I and cell proliferation, and induces cell apoptosis. BTT-3033 can be used in the research of prostate cancer, inflammation and cardiovascular disease.
    BTT-3033
  • HY-15701
    Leukadherin-1
    		Agonist 98.0%
    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.
    Leukadherin-1
  • HY-108831A
    Natalizumab (Anti-CD49d)
    		Inhibitor 99.71%
    Natalizumab (Anti-CD49d) (AN100226; BG00002) Solution is a humanized monoclonal IgG4 antibody inhibitor that selectively targets α4 integrin (CD49d), blocking the interaction of integrins such as α4β1 (VLA-4) with vascular cell adhesion molecule VCAM-1, intercellular adhesion molecule ICAM-1, and fibronectin by competitively binding to the α4 subunit. Natalizumab solution inhibits the adhesion, retention, and transendothelial migration of immune cells (such as CD4+ T cells), reducing the infiltration of inflammatory cells into the central nervous system or lesion sites, thereby exerting anti-inflammatory and immunomodulatory activity. Natalizumab (Anti-CD49d) solution is used in the study of relapsing-remitting multiple sclerosis (RRMS) and is also applied in the research of autoimmune or inflammation-related diseases such as Crohn's disease, B-cell lymphoma, and non-infectious uveitis. Natalizumab (Anti-CD49d) can also prevent lymphocytes from entering the central nervous system, thus preventing acute demyelinating relapses.
    Natalizumab (Anti-CD49d)
  • HY-P990764
    Sigvotatug
    		Ligand 99.67%
    Sigvotatug (SGN-B6A antibody) is a human IgG1 κ monoclonal antibody against ITGB6. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001). Sigvotatug can be used as an ADC antibody to synthesize ADC Sigvotatug vedotin (HY-164957).
    Sigvotatug
  • HY-P9934
    Abciximab
    		Inhibitor 99.97%
    Abciximab (C7E3), a chimeric mouse/human monoclonal antibody fragment, is a glycoprotein (GP) IIb/IIIa inhibitor. Abciximab inhibits platelet aggregation and leucocyte adhesion by binding to the glycoprotein IIb/IIIa, vitronectin and Mac-1 receptors.
    Abciximab
  • HY-100563A
    Cyclo(RGDyK)
    		Inhibitor 99.83%
    Cyclo(RGDyK) is a potent and selective αVβ3 integrin inhibitor with an IC50 of 20 nM.
    Cyclo(RGDyK)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Integrin Isoform Comparison

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