αvβ3 integrin

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.

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.

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.

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

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.

Cilengitide is a potent integrin inhibitor for αvβ3 receptor and αvβ5 receptor with IC50 of 4.1 nM and 79 nM in cell-free assays, respectively; ~10-fold selectivity against gpIIbIIIa. Phase 2.

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

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

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.

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

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.

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

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.

αvβ1integrin-IN-3 is a selective inhibitor of αvβ1 integrin, exhibiting antifibrotic properties.

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

Integrin-IN-2 is an orally bioavailable pan αv integrin inhibitor.Integrin-IN-2 can increases the αvβ6, αvβ3, αvβ5 and αvβ8 binding affinities with pIC50 values of 7.8, 8.4, 8.4 and 7.4, respectively.

GSK 3008348 hydrochloride is an αvβ6 integrin inhibitor used to confirm idiopathic pulmonary fibrosis.

Integrin Antagonists 27, a small molecule integrin αvβ3 antagonist with a binding affinity of 18 nM, serves as a novel anticancer agent.

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.

AB-3PRGD2 is a radiolabeled agent that targets integrin αvβ3. It enhances tumor uptake and prolongs retention time in tumors, significantly improving the inhibition of tumor growth. AB-3PRGD2 also remodels the tumor immune microenvironment by upregulating PD-L1 expression and increasing tumor-infiltrating CD8+ T cells.

RGD-DA6 is an αvβ3-targeting ligand composed of RGDfK (an RGD peptide targeting integrin αvβ3), DOTADG, d-Glu, Lys, AMBA, and IPBA. Through radiolabeling, RGD-DA6 forms an αvβ3-targeted radioligand for high-contrast tumor imaging and improved anticancer efficacy.

α5β1integrin-IN-1 (compound 65) is a potent and selective α5β1 integrin inhibitor with a pIC50 of 9.4. Its selectivity for α5β1 is over 10,000 times greater than for αVβ3 (pIC50 of 5.5). This compound reduces airway smooth muscle (ASM) tension by disrupting intercellular connections. In rodents, α5β1integrin-IN-1 demonstrates excellent inhalation pharmacokinetic properties and is applicable in asthma research.

JNJ-26076713, an orally active alpha V integrin antagonist, represents a potential therapeutic candidate for the treatment of macular edema, age-related macular degeneration, and proliferative diabetic retinopathy.