αvβ6

αvβ6-IN-2 (compound 20) is an effective orally active inhibitor of αvβ6 integrin (αvβ6integrin), with a pIC50 value of 7.8. It shows potential for use in research on idiopathic pulmonary fibrosis.

αvβ6-IN-1 (compound 28) is an effective orally active inhibitor of αvβ6 integrin (αvβ6integrin), with a pIC50 value of 8.1. This compound shows potential for research in idiopathic pulmonary fibrosis.

αvβ6 Integrin Inhibitor 2 is a potent inhibitor of αvβ6 integrin, demonstrating an inhibition concentration (IC50) of 96.5 nM.

EMD 527040 hydrochloride is an effective integrin αVβ6 inhibitor. The IC 50 values of EMD 527040 hydrochloride were 6 nM and 1.6 μM to inhibit αVβ6 binding to fibronectin and αVβ6 expression cells to fibronectin, respectively. EMD 527040 hydrochloride shows antifibrotic activity in animal models of biliary fibrosis and is active in vivo.

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.

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

GSK3335103 is a non-peptide, orally active inhibitor of αvβ6 integrin (pIC50=8), employed in the study of pulmonary fibrosis.

c(avb6)-DOTA TFA is a conjugate formed by the coupling of a selective αvβ6 integrin cyclic peptide and a DPTA chelating agent. The Lu (III) complex of c(avb6)-DOTA TFA exhibits considerable affinity for αvβ6 integrin (IC50=0.8 nM), making it suitable for tumor diagnostics.

MORF-627 is an orally active selective inhibitor of integrin αvβ6 (integrinαvβ6), with an IC50 of 9.2 nM as measured in a human serum ligand binding assay. It effectively inhibits αvβ6-mediated activation of TGF-β1 with an IC50 of 2.63 nM and suppresses SMAD2 3 phosphorylation, showing an IC50 of 8.3 nM. Additionally, MORF-627 ameliorates bleomycin-induced pulmonary fibrosis in mice.

Bexotegrast (PLN-74809) is an orally active and potent inhibitor of αvβ6 and αvβ1 integrins with antifibrotic effects, inhibiting αvβ6 and αvβ1-induced activation of TGF-β. It is applicable for studies of idiopathic pulmonary fibrosis (IPF) and non-specific interstitial pneumonia (NSIP).

EMD527040 is a powerful and highly specific αvβ6 antagonist, exhibiting notable antifibrotic properties. It is suitable for conducting research on carcinoma and liver fibrosis.

Bexotegrast, also known as PLN-74809, is a small-molecule, dual selective inhibitor of αVβ1 αVβ6 for idiopathic pulmonary fibrosis (IPF) and primary sclerosing cholangitis (PSC). These integrins cause upstream activation of TGF-β1 in actively fibrotic tissue. Inhibition of these integrins will block TGF-β1 activation, thereby preventing the growth of fibrotic tissue within the lung and bile ducts.

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.

A20FMDV2, a peptide derived from the α-helical RGD cell-interacting domain of the VP1 capsid protein of foot-and-mouth disease virus (FMDV) serotype O, targets and binds αVβ6 integrin. It effectively disrupts αVβ6 integrin-mediated cell adhesion in H357 tongue squamous cell carcinoma cells that exhibit human αVβ6, with an inhibitory concentration (IC50) of 1.2 µM. Additionally, when labeled with 111indium-DTPA, A20FMDV2 (20 MBq) specifically attaches to αVβ6 integrin in a breast cancer mouse xenograft model using MCF10CA1a cells, facilitating targeted radiation imaging analysis.

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.

STX-100 is a humanized antibody targeting integrin αvβ6 (ITGAV & ITGB6) with anti-tumor activity, inhibits pSMAD2, inhibits the conversion of fibroblasts to myofibroblasts, and can be used to study idiopathic pulmonary fibrosis (IPF).

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.

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.

DOTA-ADIBO TFA is a DOTA-derived bifunctional chelating agent (BFC) that facilitates drug conjugation through a catalyst-free, copper-free click reaction. It enables the construction of fusion chelator systems, and after Cu[64] modification, it is used for the synthesis of radiotracers. It is applied in positron emission tomography (PET) imaging of tumors expressing integrin αvβ6.