αvβ5 integrin

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.

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].

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.

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

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.

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].

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.

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

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.

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.