2. Signaling Pathways
  3. Cytoskeleton
  4. Integrin
  5. Integrin Antagonist

Integrin Antagonist

Integrin Isoform Comparison

Integrin Antagonists (56):

Cat. No. Product Name Effect Purity
  • 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.
  • 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.
  • 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-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.
  • 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.
  • HY-17369B
    Tirofiban
    		Antagonist 99.88%
    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.
  • HY-P9911
    Vedolizumab
    		Antagonist 99.64%
    Vedolizumab is a humanized IgG1 monoclonal antibody that targets the α4β7 integrin for the treatment of ulcerative colitis and Crohn's disease.
  • HY-124290
    Carotegrast methyl
    		Antagonist 98.89%
    Carotegrast methyl (AJM300) is an orally active and selective α4 integrin antagonist. HCA2969, an active metabolite of Carotegrast methyl, is a specific and dual α4β1/α4β7 integrin antagonist. Carotegrast methyl prevents the development of colitis in mice.
  • HY-108831
    Natalizumab
    		Antagonist ≥99.10%
    Natalizumab is a recombinant, humanized IgG4 monoclonal antibody, binds to α4β1-integrin and blocks its interaction with vascular cell adhesion molecule-1 (VCAM-1). Natalizumab can be used for the treatment of relapsing remitting multiple sclerosis and Crohn's disease. Natalizumab is also the first targeted therapy which blocks an essential mechanism for lymphocyte entry to the CNS and thus prevents acute demyelinating relapses.
  • HY-W008859
    Tetrac
    		Antagonist 98.04%
    Tetrac (Tetraiodothyroacetic acid), a derivative of L-thyroxine (T4), is a thyrointegrin receptor antagonist. Tetrac blocks the actions of T4 and 3,5,3'-triiodo-L-thyronine (T3) at the cell surface receptor for thyroid hormone on integrin αvβ3. Tetra has anti-angiogenic and anti-tumor activities.
  • HY-17369
    Tirofiban hydrochloride monohydrate
    		Antagonist 99.34%
    Tirofiban (L700462) hydrochloride monohydrate 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 monohydrate induces proliferation and migration on endothelial cell by inducing production of VEGF. Tirofiban hydrochloride monohydrate can significantly reduces myocardial no-reflow and ischemia-reperfusion injury by alleviating myocardial microvascular structural and endothelial dysfunction in the ischemic area.
  • HY-14951
    Firategrast
    		Antagonist 99.62%
    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-15770
    TR-14035
    		Antagonist 98.06%
    TR-14035 is a orally active dual α4β7/α4β1 integrin antagonist, with IC50 s of 7 nM and 87 nM for α4β7 and α4β1, respectively. TR-14035 can be used for the research of inflammation and autoimmune diseases.
  • HY-19767A
    GSK 3008348 hydrochloride
    		Antagonist 99.27%
    GSK 3008348 hydrochloride 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 GSK 3008348 (hydrochloride) is 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).
  • HY-P9911A
    Vedolizumab (anti-α4β7-integrin)
    		Antagonist 99.90%
    Vedolizumab (anti-α4β7-integrin) is a humanized IgG1 monoclonal antibody that targets the α4β7 integrin for the treatment of ulcerative colitis and Crohn's disease.
  • HY-19307
    SB-273005
    		Antagonist 99.94%
    SB-273005 is a potent nonpeptide and orally active integrin antagonist with Kis of 1.2 nM and 0.3 nM for αvβ3 receptor and αvβ5 receptor, respectively.
  • 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.
  • 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.
  • HY-138542
    RO0270608
    		Antagonist 98.80%
    RO0270608, the active metabolite of R411, is a dual alpha4beta1-alpha4beta7 (α4β1/α4β7) integrin antagonist. Antiinflammatory activity.
  • 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.