integrin β-1

αvβ1 integrin-IN-1 is a potent and selective inhibitor of αvβ1 integrin (IC50 of 0.63 nM) with antifibrotic effects.

Integrin modulator 1 is a potent and selective α4β1 integrin agonist with an IC50 value of 9.8 nM for RGD-binding α4β1. Integrin modulator 1 enhances cell adhesion mediated by α4β1 integrin with an EC50 of 12.9 nM, highlighting its utility in studying integrin-dependent adhesion processes.

αvβ1 integrin-IN-1 TFA is an effective and selective αvβ1 integrin inhibitor (IC50: 0.63 nM).

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

αLβ2integrin-IN-1 (example 1) is an inhibitor of cell adhesion mediated by αLβ2 integrin and can be utilized for studying inflammatory conditions associated with αLβ2 integrin.

αMβ2integrinagonist-1 (Compound 8) is a highly selective αMβ2 integrin agonist with anti-inflammatory properties (EC50=1.4 nM). It activates integrin-mediated cell adhesion and the JNK/ERK signaling pathway. Additionally, αMβ2integrinagonist-1 induces polarization of tumor-associated macrophages and enhances antitumor T-cell immune responses. This compound holds potential for research in cancer and chronic inflammatory diseases such as pancreatic cancer and rheumatoid arthritis.

α5β1integrin agonist-2 (Compound 2) is a highly selective agonist of the α5β1 integrin, with an EC50 of 45.98 nM. It enhances extracellular matrix adhesion and activates the Akt/ERK signaling pathways. This compound shows potential for research in ischemic stroke.

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

α5β1 integrin agonist-1 is an α5β1 integrin agonist that selectively delivers 5-FU to tumour cells and induces tumour cell death.

αvβ1 integrin-IN-2 (compound 32) is a potent inhibitor of ανβ1 and α5β1 integrins, exhibiting IC50 values of 0.9 nM and 33 nM, respectively. This compound also inhibits other integrins with IC50 values of 380 nM (ανβ3), 280 nM (ανβ5), 230 nM (ανβ6), and 87 nM (ανβ8), as determined by the SPRA assay [1].

α7β1 Integrin Modulator-1 is a potent modulator with research potential for muscular dystrophy [1].

Anti-Mouse LPAM-1/Integrinα4β7 Antibody (DATK32) is a rat-derived IgG2a, κ antibody inhibitor targeting mouse LPAM-1/Integrinα4β7.

α2β1 Integrin Ligand Peptide TFA interacts with integrin receptors on the cell membrane, mediating extracellular signaling and potentially acting as an antagonist of the collagen receptor.

The Asp-Gly-Glu-Ala (DGEA) amino acid domain of type I collagen interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors.

α2β1 Integrin Ligand Peptide acetate (α2β1 Integrin Ligand Peptide acetate (134580-64-6)) is a potential antagonist of α2β1 integrin receptor. α2β1 Integrin Ligand Peptide interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells.

Nexinhib20 is an inhibitor of exosome synthesis and transport with anti-inflammatory activity, inhibits RAB27A and neutral sphingomyelinase 2 (nSMase2) nsMase2, inhibits IL-8-induced β(2) integrin-dependent adhesion of human neutrophils in the subfluidic phase, and inhibits neutrophil adhesion and β(2) integrin activation through antagonism of the rac-1-guanosine 5'-triphosphate interaction. beta(2) integrin activation.

XVA143 is an integrin α/β I-like allosteric antagonist that inhibits LFA-1 (αLβ2 integrin)-dependent firm adhesion and induces an extended conformation of integrins.

1. Glaucocalyxin A (Leukamenin F)-SBE-β-CD could be useful with a better solubility and sustained function in drug delivery. 2. Glaucocalyxin A activates caspase-3, decreases BAD phosphorylation, and reduces the expression of X-linked inhibitor of apoptosis protein. 3. Glaucocalyxin A inhibits Akt phosphorylation, suppresses proliferation, and promotes apoptosis in a dose-dependent manner, but not in normal glial cells. 4. Glaucocalyxin A inhibits collagen-stimulated tyrosine phosphorylation of Syk, LAT, and phospholipase Cγ2, the signaling events in collagen receptor GPⅥ pathway. 5. Glaucocalyxin A could potentially be developed as an antiplatelet and antithrombotic agent, can inhibit platelet p-selectin secretion and integrin activation by convulxin, is a GPVI selective ligand.

mP6 (Myr-FEEERA-OH), a myristoylated peptide, selectively inhibits Gα 13's interaction with integrin β 3 while preserving talin-dependent integrin function. Additionally, mP6 impedes the GTPase activity of Rac1, Rap1, and Rab7, effectively reducing the infection of CHO-A24 cells [1].

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].

N-Acetylgalactosaminyltransferase 1 (GALNT1) is a glycosyltransferase that initiates mucin-type O-glycosylation by transferring α-GalNAc from UDP-GalNAc to serine (Ser) or threonine (Thr) residues in proteins. Overexpression of N-Acetylgalactosaminyltransferase 1 in gastric cancer enhances the aberrant O-glycosylation of CD44, activating the Wnt/β-catenin signaling pathway and influencing the malignant behavior of gastric cancer cells. This enzyme plays a crucial role in cancer progression and metastasis by modifying the O-glycosylation of various glycoproteins such as mucin (MUC1), osteopontin (OPN), matrix metalloproteinase-14 (MMP14), and integrin α3.