β1 integrin

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

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.

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.

α5β1integrin-IN-1 (compound 65) is a potent and selective α5β1 integrin inhibitor with a pIC50 of 9.4. Its selectivity for α5β1 is over 10,000 times greater than for αVβ3 (pIC50 of 5.5). This compound reduces airway smooth muscle (ASM) tension by disrupting intercellular connections. In rodents, α5β1integrin-IN-1 demonstrates excellent inhalation pharmacokinetic properties and is applicable in asthma research.

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].

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.

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

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.

α4β7Integrin-IN-1 (Example 356) is a potent inhibitor of the α4β7 integrin, effectively blocking the interaction between α4β7 integrin and MadCAM-1 with an EC50 of 0.05 nM. This compound is utilized in research related to inflammatory bowel disease.

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.

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

α7β1 integrin modulator-1 is an α7β1 integrin activator. It upregulates α7 integrin expression and enhances laminin binding, utilized in Duchenne Muscular Dystrophy (DMD) research.

RO0270608, the active metabolite of R411, is an orally active dual α4β1/α4β7 integrin antagonist with anti-inflammatory properties, useful for studying allergic inflammatory responses.

Firategrast (SB 683699) is an orally active and specific α4β1/α4β7 integrin antagonist that reduces the transport of lymphocytes into the central nervous system (CNS) and decreases multiple sclerosis (MS) activity. It is used in relapsing-remitting multiple sclerosis, associated with modest reductions in CD4, CD8, and CD19 lymphocyte counts in cerebrospinal fluid.

Pyrintegrin, a β1-integrin agonist, promotes the survival of embryonic stem cells, can be used as a podocyte-protective agent, and enhances cell-extracellular matrix adhesion-mediated integrin signaling.

DIM-C-pPhOH (CDIM8) is a nur77 (NR4A1) antagonist,inhibits TGF-β induced cell migration of breast cancer cell lines,promotes ROS/endoplasmic reticulum stress and proapoptotic pathways in pancreatic cancer cell lines,mimics effects of Nur77 RNAi silencing.

Natalizumab is a recombinant humanized monoclonal antibody and a humanized monoclonal antibody inhibitor that selectively targets α4 integrin (CD49d). Natalizumab binds to the α4β1 heterodimer and blocks its interaction with vascular cell adhesion molecule 1. Natalizumab also prevents lymphocytes from entering the central nervous system, thereby preventing acute demyelinating relapses, and is used in the study of relapsing-remitting multiple sclerosis and Crohn’s disease. Natalizumab possesses anti-inflammatory and immunomodulatory activity, inhibiting the adhesion, retention, and transendothelial migration of immune cells, and reducing the infiltration of inflammatory cells into the central nervous system or affected sites. Natalizumab is also being studied for autoimmune or inflammation-related diseases such as B-cell lymphoma and non-infectious uveitis.

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

BIO-1211 is a more potent inhibitor of α4β1 (VLA-4, IC50 = 4 nM) over α4β7(IC50 = 2 μM).