integrins

Tyrphostin AG957, a tyrosine kinase inhibitor with anti-BCR/ABL tyrosine kinase activity restores beta1 integrin-mediated adhesion and inhibitory signaling in chronic myelogenous leukemia hematopoietic progenitors[1].

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.

Integrin signaling inhibitor, mP13 is a compound that inhibits integrin signaling, blocks inside-out and outside-in signaling, and is involved in fibrinogen binding, platelet adhesion, and clot contraction.

GRGDSPK acetate shows inhibitory activity against integrin-fibronectin binding and can be used in research on integrins in bone formation and resorption.

Arg-Gly-Asp-Ser (RGDS peptide) is a conserved tetrapeptide sequence found on fibronectin, fibrinogen α, and von Willebrand factor. It binds to integrins on the cell surface, inhibiting thrombin-induced platelet-fibrinogen interaction.

Carotegrast is a selective α4 integrin antagonist that inhibits the migration of inflammatory cells to the intestinal mucosa by blocking the interaction between α4β1/α4β7 integrins and their ligands. Carotegrast is used in research and clinical practice for the treatment of inflammatory bowel diseases such as ulcerative colitis; it exerts local anti-inflammatory effects and results in low systemic exposure.

SB-267268 inhibits human and mouse αvβ3 (IC50s: 0.68 and 0.29 nM, respectively). SB-267268 is a selective and nonpeptidic alpha(v)beta3 and alpha(v)beta5 integrins antagonist (Kis: 0.9, 0.5 and 0.7 nM for human αvβ3, monkey αvβ3 and human αvβ5, respective

SF1126 is a relevant pan and dual first-in-class PI3K/BRD4 inhibitor. An RGDS-conjugated LY294002 prodrug, it is designed for increased solubility and specifically binds to integrins within the tumor compartment.

Zaurategrast (CDP323) is a small-molecule prodrug antagonist that inhibits the interaction between vascular cell adhesion molecule 1 (VCAM-1) and α4-integrins, originally developed by Celltech plc for oral administration, and it serves as a valuable research compound for investigating leukocyte trafficking, immune cell adhesion, and therapeutic strategies relevant to multiple sclerosis.

BOP is anantagonist of alpha4beta1/alpha9beta1 integrins. BOP rapidly mobilizes long-term multi-lineage reconstituting hematopoietic stem cells (HSC).

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.

Echistatin TFA, the smallest active RGD protein from snake venoms, is a potent inhibitor of platelet aggregation, bone resorption in culture, and an antagonist of αIIbβ3, αvβ3, and α5β1[1][2][3][4].

BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd < 10 pM). The compound selectively binds to α4β1 (IC50 = 1.8 nM) over various other integrins and results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels[1][2].

THI0019 is a highly potent agonist of the integrin α4β1 (VLA-4) receptor, with an EC 50 range of 1-2 μM. It effectively promotes the adhesion of stem/progenitor cells. Furthermore, THI0019 successfully modulates adhesion processes mediated by α4β7, α5β1, and αLβ2 integrins.

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).

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.

Integrin Binding Peptide acetate is a synthetic peptide derived from the fibronectin protein that selectively binds integrins. Integrin Binding Peptide acetate can be employed as a functional biomolecule in the preparation of PEG-based hydrogels, providing a biologically active interface for cell adhesion, migration, and mechanotransduction studies in tissue engineering and regenerative medicine.

BOP-JF549 is a fluorescent dual α9β1/α4β1 integrin inhibitor. Comprises BOP conjugated to Janelia Fluor® 549. Fluorogenic: fluoresces only once bound to integrins, enabling hassle-free no-wash experiments. Bright and photostable, enabling live cell tracking of integrin receptors over long time-course experiments. Excitation maximum = 549 nm; emission maximum = 571 nm.

BOP-JF646 is a fluorescent dual α9β1/α4β1 integrin inhibitor. Comprises BOP conjugated to Janelia Fluor®646. Fluorogenic: fluoresces only once bound to integrins, enabling hassle-free no-wash experiments. Bright and photostable, enabling live cell tracking of integrin receptors over long time-course experiments. Excitation maximum = 655 nm; emission maximum = 672 nm.

Arg-Gly-Asp TFA (99896-85-2(free base)) (RGD Trifluoroacetate) is a tripeptide that effectively triggers cell adhesion, addresses certain cell lines and elicits specific cell responses; binds to integrins.

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

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.

Arginine-glycine-aspartic acid

Cilengitide hydrochloride sis the salt form of Cilengitide, a cyclic Arg-Gly-Asp peptide with potential antineoplastic activity. Cilengitide binds to and inhibits the activities of the alpha(v)beta(3) and alpha(v)beta(5) integrins, thereby inhibiting endothelial cell-cell interactions, endothelial cell-matrix interactions, and angiogenesis.