α5β1

α5β1 integrin agonist-1 is an α5β1 integrin agonist that selectively delivers 5-FU to tumour cells and induces tumour cell death.

K34c hydrochloride is an alpha5β1 integrin antagonist for glioblastoma study.

CLT-28643 is a potent and specific α5β1-Integrin inhibitor that prevents fibrosis in glaucoma filtration surgery (GFS), inhibits tumor growth and angiogenesis, suppresses fibrosis and inflammation in a bleomycin-induced lung fibrosis model, and improves insulin sensitivity and cardiac function in H9C2 cells from obese mice.

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.

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.

ATN-161, a novel integrin α5β1 antagonist, inhibits angiogenesis and the growth of liver metastases in a murine model.

c (phg-isoDGR- (NMe) k) is a selective and effective α5β1-integrin ligand with IC50 of 2.9 nM.

c(phg-isoDGR-(NMe)k) TFA is a potent and selective α5β1-integrin ligand (IC50: 2.9 nM).

MK-0429 is an orally active, selective, and nonpeptide antagonist of αvβ3 integrin (IC50: 80 nM).

LT25 (compound 17) acts as an agonist for the α5β1 integrin, exhibiting an EC50 value of 9.9 nM.

Echistatin TFA, the smallest active RGD protein from snake venoms, is a potent inhibitor of platelet aggregation, bone resorption in culture, and an antagonist of αIIbβ3, αvβ3, and α5β1[1][2][3][4].

THI0019 is a highly potent agonist of the integrin α4β1 (VLA-4) receptor, with an EC 50 range of 1-2 μM. It effectively promotes the adhesion of stem/progenitor cells. Furthermore, THI0019 successfully modulates adhesion processes mediated by α4β7, α5β1, and αLβ2 integrins.

K34c is a potent and selective α5β1 integrin inhibitor (IC50 = 3.1 nM) that inhibits cell survival and migration, p53-dependent senescence induced by Temozolomide or Ellipticine, and promotes apoptosis in U87MG cells. Additionally, K34c prevents TGFβ-induced infiltration [in vivo] and reduces cell adhesion on fibronectin.

C(phg-isoDGR-(NMe)k) TFA is a selective and potent ligand for α5β1-integrin, exhibiting an IC50 of 2.9 nM [1].

RGD peptide (GRGDNP) TFA functions as an inhibitor of integrin-ligand interactions, competitively blocking α5β1's interaction with the extracellular matrix (ECM). It induces apoptosis by triggering conformational changes that facilitate pro-caspase-3 activation and autoprocessing. Furthermore, RGD peptide (GRGDNP) TFA is critical in regulating cell adhesion, migration, growth, and differentiation [1] [2] [3].

αvβ1 integrin-IN-2 (compound 32) is a potent inhibitor of ανβ1 and α5β1 integrins, exhibiting IC50 values of 0.9 nM and 33 nM, respectively. This compound also inhibits other integrins with IC50 values of 380 nM (ανβ3), 280 nM (ανβ5), 230 nM (ανβ6), and 87 nM (ανβ8), as determined by the SPRA assay [1].

Cyclo(Gly-Arg-Gly-Asp-Ser-Pro) (c(GRGDSP)) is an RGD-containing inhibitory peptide and synthetic α5β1 integrin ligand that competitively inhibits the binding of invasin (Inv) to α5β1 integrin on Caco-2 cells [1].

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.

RGD Trifluoroacetate is a tripeptide that effectively triggers cell adhesion, targets specific cell lines, and elicits particular cell responses by binding to integrins. It is the most effective and frequently used peptide sequence for stimulated cell adhesion on synthetic surfaces. Among the 24 integrins that bind to ECM molecules in an RGD-dependent manner are α3β1, α5β1, α8β1, αIIbβ3, αvβ1, αvβ3, αvβ5, αvβ6, αvβ8, and to some extent α2β1 and α4β1.

C16Y, a short peptide, serves as an inhibitor for the integrins αvβ3 and α5β1. It targets the cell membrane and exerts its antitumor activity by inhibiting angiogenesis.