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.