αvβ3 integrin

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.

Cyclo(RGDyK) is a potent and selective αVβ3 integrin inhibitor with an IC50 of 20 nM.

Potent irreversible αVβ3 integrin antagonist (Ki = 0.27 nM). Disrupts attachment of osteoclasts to bone and inhibits bone reabsorption (IC50 = 0.1 nM). Prevents ADP-induced platelet aggregation via inhibition of glycoprotein IIb IIIa (GpIIb IIIa, αIIbβ3)

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.

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

LXW7 TFA, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor with an anti-inflammatory effect. LXW7 has a high binding affinity to αvβ3 integrin (IC50: 0.68 μM). It increases the phosphorylation of VEGFR-2 and activation of ERK1 2.

Arg-Gly-Asp-Ser acetate is an integrin binding sequence that 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 acetate inhibits integrin receptor function.

Cyclo(Arg-Gly-Asp-D-Phe-Val) is an integrin αvβ3 inhibitor with antitumor properties, used in acute myeloid leukemia research [1].

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(RGDfC) TFA (Cyclo(Arg-Gly-Asp-D-Phe-Cys) TFA) is a cyclic pentapeptide, a cyclic RGD polypeptide with high affinity for αvβ3, which is capable of disrupting cellular integrin interactions. Cyclo(RGDfC) TFA inhibits pluripotent gene expression in embryonic stem cells (ESCs) and inhibits tumorigenic potential of mESCs in vivo. Cyclo(RGDfC) TFA inhibits the tumorigenic potential of mESC. Cyclo(RGDfC) TFA can be used for tumor-related studies.

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

Potent antagonist of the integrin αvβ3-vitronectin interaction (IC50 = 25.72 nM). Blocks proliferation and induces apoptosis in HUVECs; antiangiogenic.

Gly-Arg-Gly-Asp-Ser (GRGDS) acetate is a cell binding protein domain derived from the cell-binding region of fibronectin.

Maraciclatide is a radiopharmaceutical targeting αvβ3 integrin.

Cyclo(RGDyK) trifluoroacetate is a potent and selective αVβ3 integrin inhibitor with an IC50 of 20 nM.

Arg-Gly-Asp-D-Phe-Val (TFA) has anti-tumor activity and is an inhibitor of integrin αvβ3.

DOTA-cyclo(RGDfK) is a and DOTA-like chelator peptide consisting of a dimer of the peptide cross-linker DOTA and the cyclic peptide RGDFK, which preferentially targets the αvβ3 integrin receptor expressed on tumor cell membranes, allowing for the preparation of radionuclide coupled compounds (RDCs) and their use in cancer diagnostics and therapy.

HSDVHK-NH2 TFA acts as an antagonist to the αvβ3-vitronectin integrin interaction, displaying an inhibitory concentration (IC 50) of 1.74 pg mL (2.414 pM) [1] [2].

Highly potent integrin α1β1 inhibitor (IC50 = 0.8 nM for α1β1 binding to type IV collagen). Selective for α1β1 over α2β1, αIIbβ3, αvβ3, α4β1, α5β6, α9β1 and α4β7. Inhibits FGF2-stimulated angiogenesis in the chicken chorioallantoic model. Displays antitum

RTDLDSLRTYTL is a ligand for αVβ6 integrin, exhibiting selective inhibition of fibronectin's binding to αVβ6 integrin with considerably less effect on the interactions between vitronectin and αVβ3 or αVβ5, as well as fibrinogen and αIIβ3 (IC50s = 0.02, >50, >50, and >50 µM, respectively). Additionally, it prevents HT-29 colon cancer cells from binding to fibronectin in a concentration-dependent fashion.

E(c(RGDfK)) is an αvβ3 integrin-specific binding moiety with tumor-targeting properties, demonstrating increased uptake in human ovarian cancer OVCAR-3 xenograft tumors, suggesting potential utility in cancer research [1].