Integrin

Tirofiban(MK383) hydrochloride monohydrate is a non-peptide glycoprotein IIb IIIa antagonist.

Teclistamab (JNJ-64007957) is a human bispecific monoclonal antibody targeting the CD3 receptor expressed on the surface of t-cells and the b-cell maturation antigen (BCMA) expressed on the surface of malignant multiple myeloma b-lineage cells for the treatment of relapsed and refractory multiple myeloma.

Natalizumab used for the treatment of relapsing remitting multiple sclerosis and Crohn's disease.

GLPG0187, a broad spectrum integrin receptor antagonist, inhibits αvβ1-integrin (IC50: 1.3 nM).

BTT-3033 is an orally active and potent α2β1 (EC50: 130 nM) inhibitor with an affinity for the α2I domain, inhibiting platelet binding to collagen I and cell proliferation. BTT-3033 induces apoptosis and can be used to study prostate cancer, inflammation, and cardiovascular disease.

PLN-1474 is a potent αVβ1 inhibitor with IC50 < 50 nM.

Cyclo(-RGDfK) is a potent and selective inhibitor of integrin αvβ3 with IC50 of 0.94 nM. Cyclo specifically targets tumor microvasculature and cancer cells by binding to αvβ3 integrin on the cell surface.

Cyclo(-RGDfK) is a selective αvβ3 integrin inhibitor(IC50 : 0.94 nM).

Cucurbitacin B (Cuc B) has profound in vitro and in vivo antiproliferative effects against human pancreatic Y cells. It inhibited AKT signaling activation through up-regulation of PTEN. Cucurbitacin B is an effective inhibitor of HIF-1 and provide new perspectives into the mechanism of its anticancer activity. Cucurbitacin B inhibits proliferation and induces apoptosis via STAT3 pathway inhibition in A549 lung Y cells.

Cilengitide (EMD 121974) is a potent integrin inhibitor for the αvβ3 5 receptor (IC50: 4.1 79 nM, in cell-free assays) with approximately 10-fold selectivity against gpIIbIIIa.

iRGD peptide (c(CRGDKGPDC)) is a 9-amino acid cyclic peptide (sequence: CRGDKGPDC) and a molecular mimicry agent that was originally identified in an in vivo screening of phage display libraries in tumor-bearing mice.

Roxifiban acetate(DMP 754 acetate) is a potent GP IIb IIIa antagonist that exhibits antiplatelet aggregation activity via immune mediation and can be used in the study of human thrombocytopenia.

Bestatin hydrochloride (Ubenimex hydrochloride) is an inhibitor of aminopeptidase N (APN) CD13 and aminopeptidase B.

ICAM-1-IN-1 is a potent and selective inhibitor of E-selectin (IC50 = 7 nM) and ICAM-1 (IC50 = 5 nM).

ATN-161 trifluoroacetate salt (ATN-161 TFA salt) is a novel integrin α5β1 antagonist that inhibits angiogenesis and growth of liver metastases and improves survival in a murine model.

Vedolizumab, a humanized monoclonal antibody, targets the α4β7 integrin for treating Crohn's disease and ulcerative colitis.

Carotegrast methyl (AJM300), an orally-active small molecule, can antagonize the α4 integrin receptor. It is a specific and dual α4β1 α4β7 integrin antagonist.

SB273005 is an orally active and potent nonpeptide integrin αvβ3 antagonist that inhibits αvβ3 and αvβ5 and reduces the production of Th2 cells and the cytokine IL-10 in pregnant mice.

CWHM-12 is a potent inhibitor of αV integrins, with IC50 values of 0.2, 0.8, 1.5, and 1.8 nM for αvβ8, αvβ3, αvβ6, and αvβ1, respectively.

BIRT-377 is a negative allosteric and orally bioavailable inhibitor of ICAM-1 and LFA-1(Ki = 25.8 nM). BIRT-377 inhibits the production of IL-2 and can be used in studies about inflammatory and immune disorders.

E7820 (ER68203-00) is an angiogenesis inhibitor by suppressing integrin a2 (a cell adhesion molecule expressed on endothelial cells).

αvβ1 integrin-IN-1 is a potent and selective inhibitor of αvβ1 integrin (IC50 of 0.63 nM) with antifibrotic effects.

Volociximab (M200) is an IgG4 monoclonal antibody targeting the α5β1 integrin , with antiangiogenic, antitumor and anticancer activity, inhibits the growth of rabbit VX2 tumors and is used to study solid tumors.

RO0270608, the active metabolite of R411, is an orally active dual α4β1 α4β7 integrin antagonist with anti-inflammatory properties, useful for studying allergic inflammatory responses.

Pyrintegrin, a β1-integrin agonist, promotes the survival of embryonic stem cells, can be used as a podocyte-protective agent, and enhances cell-extracellular matrix adhesion-mediated integrin signaling.

BIO-1211 is a more potent inhibitor of α4β1 (VLA-4, IC50 = 4 nM) over α4β7(IC50 = 2 μM).

Abciximab (C7E3) is a mouse human chimeric monoclonal antibody that is a potent glycoprotein IIb IIIa inhibitor. Abciximab has anti-platelet aggregation and leukocyte adhesion, acting by binding to glycoproteins IIb IIIa, vitronectin and Mac-1 receptors.

Irigenin mediates its antimetastatic effect by specifically and selectively blocking the α9β1 and α4β1 integrin binding sites on the C-C loop of the Extra Domain A domain. It can sensitize TRAIL-induced apoptosis by enhancing the expression of pro-apoptotic molecules in gastric cancer cells and has anti-cancer effects.

Cyclo(RADfK) is a selective α(v)β(3) integrin ligand extensively used for research, therapy, and diagnosis of neoangiogenesis. It also serves as a negative control for cyclo(-RGDfK-), the RGD peptide, which modulates cell adhesion and is recognized by several integrin family members.

Lifitegrast (SAR 1118) is an antagonist of lymphocyte function-associated antigen-1.

Vaccarin is a major flavonoid glycoside in Vaccariae semen, its biotransformation pathways involves methylation, hydroxylation, glycosylation and deglycosylation.

Arginine-glycine-aspartic acid

Blinatumomab (AMG-10,MT-103) is a CD19 CD3 bispecific B-cell and T-cell binding antibody that directs T-cells to attack cancer cells by binding to both CD3 on T-cells and CD19 on cancer cells, and is used in acute lymphoblastic leukemia and non-Hodgkin's lymphoma.

Bexotegrast (PLN-74809) is an orally active and potent inhibitor of αvβ6 and αvβ1 integrins with antifibrotic effects, inhibiting αvβ6 and αvβ1-induced activation of TGF-β. It is applicable for studies of idiopathic pulmonary fibrosis (IPF) and non-specific interstitial pneumonia (NSIP).

P11 acetate is an integrin αvβ3-vitronectin interaction antagonist(IC50 = 2.74 nM).

Tadocizumab (C4G1) is a humanized monoclonal antibody targeting integrin αIIbβ3 with antiplatelet and antithrombotic activity that blocks the platelet αIIbβ3 integrin interac- with brinogen and bronectin, and can be used in the study of cardiovascular disease.

OSU-T315 (OSU-T315 (1,5-regioisomer)) (1,5-regioisomer) is a ILK inhibitor.

ILK-IN-2 (OSU-T315) is a novel potent, orally active ILK (integrin-linked kinase) inhibitor with IC50 of 0.6 μM.

Tirofiban (L700462) (MK-383) is a selective palate GPIIb IIIa antagonist which inhibits platelet aggregation with IC50 of 9 nM.

A 286982 is an inhibitor that blocks the integrin-ligand interaction between leukocyte function-associated antigen-1 (LFA-1) and intercellular adhesion molecule-1.

2-Fluoropalmitic acid (2-Fluorohexadecanoic acid), a fatty acid containing fluorine atoms, serves as a potential therapeutic agent for glioblastoma (GBM) by inhibiting the viability, proliferation, and stem-like phenotype of glioma stem cells (GSCs), suppressing the expression of phosphorylated erk, CD133, and SOX-2, and leading to decreased MMP-2 activity and increased methylation of the MGMT promoter.

LXW7 is an octamer disulfide cyclic peptide and αvβ3 integrin ligand, acts as a potent and specific endothelial progenitor cells (EPCs) and endothelial cells (ECs) targeting ligand. LXW7 is a disulfide cyclic octa-peptide (cGRGDdvc) containing unnatural amino acids flanking both sides of the main functional motif.

Lifitegrast sodium (SAR-1118-023 sodium) is a small molecule integrin antagonist that inhibits T cell-mediated inflammation by blocking the binding of two important cell surface proteins (lymphocyte function-associated antigen 1 and intercellular adhesion molecule 1), which reduces inflammation of the ocular surface, and may be used in the study of dry eye.

3'-Demethylnobiletin has chemopreventive effects on colon carcinogenesis, it can significantly inhibit the growth of human colon cancer cells, cause cell-cycle arrest, induce apoptosis, and profoundly modulate signaling proteins related with cell prolifer

Leukadherin-1 is an allosteric activator of CD11b CD18. Increasing CD11b CD18-dependent cell adhesion to fibrinogen, Decreasing leukocyte motility and transendothelial migration; reduces inflammation.

A-205804 is a specific and effective inhibitor of E-selectin( IC50=20 nM ) and ICAM-1(IC50=25 nM) expression.

Arg-Gly-Asp TFA (99896-85-2(free base)) (RGD Trifluoroacetate) is a tripeptide that effectively triggers cell adhesion, addresses certain cell lines and elicits specific cell responses; binds to integrins.

ILK-IN-3 is an inhibitor of integrin linked kinase, and with antitumor activity.