αvβ5

αvβ5 integrin-IN-1, a potent and selective αvβ5 integrin inhibitor, exhibits a high inhibitory potency with a pIC50 value of 8.2.

αvβ5 integrin-IN-2 (Cpd_AV2) is an inhibitor that targets the β-propeller central pocket of ITGAV (integrin αV) and disrupts the stability of integrin heterodimers. This compound induces cellular apoptosis [1].

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.

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

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.

HB-3-20 induces the degradation of integrin αVβ5 on the cell surface. Transglutaminase 2 (TG2) specifically interacts with HB-3-20, exhibiting a catalytic efficiency (kcat KM) of 0.16 μM^-1min^-1.

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.

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.

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

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.

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

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.

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.

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.

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].