β1-integrin

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.

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

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.

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.

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

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

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

BTT-3033 is an orally active and potent α2β1 (EC50: 130 nM) inhibitor with an affinity for the α2I domain, inhibiting platelet binding to collagen I and cell proliferation. BTT-3033 induces apoptosis and can be used to study prostate cancer, inflammation, and cardiovascular disease.

Valategrast hydrochloride (R411), a dual antagonist of integrin α4β1 (VLA-4), is used for the potential treatment of asthma.

Carotegrast methyl (AJM300), an orally-active small molecule, can antagonize the α4 integrin receptor. It is a specific and dual α4β1/α4β7 integrin antagonist.

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).

GLPG0187, a broad spectrum integrin receptor antagonist, inhibits αvβ1-integrin (IC50: 1.3 nM).

TR-14035 (MDK-1191) is a dual antagonist of α4β7/α4β1 integrins (IC50s: 7/87nM).

PLN-1474 is a potent αVβ1 inhibitor with IC50 < 50 nM.

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

WAY-301398 is a bioactive experimental molecule primarily used for biochemical reaction research. It is frequently used as a pharmacological tool in in vitro experimental models.

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

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