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-16141
    Cilengitide
    		Antagonist 99.80%
    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.
    Cilengitide
  • 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.
    Cyclo(-RGDfK)
  • HY-N0416
    Cucurbitacin B
    		Inhibitor 99.91%
    Cucurbitacin B belongs to a class of highly oxidized tetracyclic triterpenoids and is oral active. Cucurbitacin B inhibits tumor cell growth, migration and invasion and cycle arrest, but induces cell apoptosis. Cucurbitacin B has potent anti-inflammatory, antioxidant, antiviral, hypoglycemic, hepatoprotective, neuroprotective activity.
    Cucurbitacin B
  • HY-100506
    GLPG0187
    		Antagonist 99.43%
    GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits αvβ1-integrin with an IC50 of 1.3 nM. GLPG0187 inhibits migrasome biogenesis without cytotoxicity.
    GLPG0187
  • HY-137561
    Bexotegrast
    		Inhibitor 98.94%
    Bexotegrast (PLN-74809) is an orally active, potent dual αvβ6/αvβ1 integrin inhibitor with Kd of 5.7 nM and 3.4 nM, respectively. Bexotegrast inhibits αvβ6- and αvβ1-induced TGF-β activation with IC50 values of 29.8 nM and 19.2 nM, respectively. Bexotegrast has antifibrogenic effects and block multiple avenues of TGF-β activation in the fibrotic lung.
    Bexotegrast
  • HY-NP132
    Recombinant Humanized Type III Collagen (80-100kDa)
    Recombinant Humanized Type III Collagen (80-100kDa) is a type III collagen (80-100kDa). Recombinant humanized type III collagen (rhCOLIII) has various biological functions, such as promoting skin extracellular matrix regeneration and improving the cell microenvironment. rhCOLIII inhibits the proliferation, migration, and invasion of breast cancer cells. Type III collagen functions in cell adhesion, migration, proliferation and differentiation through its interaction with integrins.
    Recombinant Humanized Type III Collagen (80-100kDa)
  • HY-P1654
    A20FMDV2
    		Inhibitor 98.03%
    A20FMDV2 is a selective αvβ6 integrin inhibitor (IC50: 3 nM), with an activity 1,000-fold more selective for αvβ6 than for other RGD-directed integrins (αvβ3, αvβ5, and α5β1). A20FMDV2 can be derived from the foot-and-mouth disease virus. A20FMDV2 can be radiolabeled for the PET imaging of αvβ6 integrin-positive tumors.
    A20FMDV2
  • HY-NP026
    Spirulina C-phycocyanin
    		Inhibitor
    Spirulina C-phycocyanin, a component of the light-harvesting phycobilisome complex in photosystem II, is a highly dominant chromoprotein in Spirulina. Spirulina C-phycocyanin can be detected by Raman spectral measurement. Spirulina C-phycocyanin has antioxidant, anti-inflammatory, antiplatelet, liver-protective and cholesterol-lowering effects.
    Spirulina C-phycocyanin
  • HY-P3160
    Fibronectin
    		Modulator
    Fibronectin, a glycoprotein 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.
    Fibronectin
  • HY-14571
    E7820
    		Inhibitor 99.06%
    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.
    E7820
  • HY-13306
    Pyrintegrin
    		Agonist 99.41%
    Pyrintegrin is an β1-integrin agonist and a 2,4-disubstituted pyrimidine that promotes embryonic stem cells survival. Pyrintegrin enhances cell-extracellular matrix (ECM) adhesion-mediated integrin signaling. Pyrintegrin can be used as a podocyte-protective agent and has robustly adipogenic.
    Pyrintegrin
  • HY-12290
    Arg-Gly-Asp-Ser
    		Inhibitor 99.93%
    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.
    Arg-Gly-Asp-Ser
  • 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-18644
    CWHM-12
    		Inhibitor 99.94%
    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.
    CWHM-12
  • HY-15102
    MK-0429
    		Antagonist 99.08%
    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-19344
    Lifitegrast
    		Antagonist 99.29%
    Lifitegrast (SAR 1118) is a potent integrin antagonist. Lifitegrast blocks the binding of intercellular adhesion molecule 1 (ICAM-1) to lymphocyte function-associated antigen 1 (LFA-1), interrupting the T cell-mediated inflammatory cycle. Lifitegrast inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. Lifitegrast can be used for researching dry eye disease.
    Lifitegrast
  • HY-P0278
    RGD
    		98.37%
    RGD is a tripeptide that effectively triggers cell adhesion, addresses certain cell lines and elicits specific cell responses; binds to integrins.
    RGD
  • HY-100445A
    αvβ1 integrin-IN-1 TFA
    		Inhibitor 98.04%
    αvβ1 integrin-IN-1 TFA (Compound C8) is a potent and selective αvβ1 integrin inhibitor with an IC50 of 0.63 nM. Antifibrotic effects.
    αvβ1 integrin-IN-1 TFA
  • HY-P0074
    GPRP
    		99.81%
    GPRP (Pefa 6003) is a fibrin polymerization inhibitor that inhibits the interaction of fibrinogen with the platelet membrane glycoprotein IIb/IIIa complex (GPIIb/IIIa).
    GPRP
  • 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.
    A-205804
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Integrin Isoform Comparison

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