αvβ3

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.

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.

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.

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.

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

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

SB-267268 inhibits human and mouse αvβ3 (IC50s: 0.68 and 0.29 nM, respectively). SB-267268 is a selective and nonpeptidic alpha(v)beta3 and alpha(v)beta5 integrins antagonist (Kis: 0.9, 0.5 and 0.7 nM for human αvβ3, monkey αvβ3 and human αvβ5, respective

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.

BGC0222 is a novel Irinotecan prodrug. As a PEG-cRGD conjugated derivative of Irinotecan, BGC0222 enables the slow and steady release of Irinotecan. It binds to the αVβ3 target with an IC50 of 4.25 μM and has an IC50 of 58.7 μM for αVβ5. BGC0222 can induce angiogenesis and demonstrates significant antitumor activity in various tumors.

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.

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].

Tetrac (Tetraiodothyroacetic acid) is a derivative of L-thyroxine (T4), a thyroxine integrin receptor antagonist.Tetrac induces antiproliferation by blocking EGFR-mediated cell signaling in colorectal cancer cells.Tetrac blocks the effects of T4 and 3,5,3'-triiodo-L-thyronine (T3) on the cell-surface thyroxine integrin αvβ3 receptors.Tetra has anti-angiogenic, anti-tumor activity and pro-apoptotic activity.

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 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).

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

D-Ornithine lactam is a building block. It has been used in the synthesis of hepatitis C virus non-structural protein 5B inhibitors, as well as αVβ3 integrin receptor antagonists.

TSRI265 is a novel αvβ3 ligand, disrupting the integrin-MMP2 interaction and showing antiangiogenic activit, inhibiting angiogenesis and tumor growth in vivo.

SF0166 is a potent, selective antagonist of α v β 3, demonstrating IC 50 values of 0.6 nM for α v β 3, 8 nM for α v β 6, and 13 nM for α v β 8. It effectively inhibits cellular adhesion to vitronectin in human, rat, rabbit, and dog cell lines, with IC 50 values ranging from 7.6 pM to 76 nM. Additionally, SF0166 significantly reduces neovascularization in the oxygen-induced retinopathy mouse model.

TC113, a Gemcitabine (GEM)-based conjugate incorporating the c(RGDyK) sequence, is internalized by A549 cells via the integrin αvβ3 pathway. It demonstrates significant antiproliferative effects on both WM266.4 and A549 cell lines.

Gly-Arg-Gly-Asp-Ser (TFA), a pentapeptide comprising the cell-binding domain of osteopontin (a glycoprotein), interacts with integrin receptors αvβ3 and αvβ5, with estimated IC50 values of approximately 5 μM and 6.5 μM, respectively [1][2].

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].