integrins

Tirofiban hydrochloride monohydrate (MK-383 Hydrochloride) is a potent non-peptide, glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) antagonist.

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.

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

Cilengitide (EMD 121974) is a potent integrin inhibitor for the αvβ3/5 receptor (IC50: 4.1/79 nM, in cell-free assays); ~10-fold selectivity against gpIIbIIIa.

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. Additionally, this compound inhibits a range of 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].

Certepetide (CEND-1), also known as iRGD, is a bifunctional cyclic peptide that enhances tumor penetration. By interacting with alphav-integrins through its RGD motif and activating NRP-1, it transforms the solid tumor microenvironment into a temporary conduit for therapeutic agents. This property facilitates Certepetide's accumulation in tumors, making it a valuable tool in researching pancreatic cancer and other solid tumors [1] [2] [3].

G-{d-Arg}-GDSP, an RGD peptide analogue, binds to the adhesion receptor of integrins, inhibiting cellular attachment to fibronectin and osteoclast resorption [1].

FN-A208 is an active peptide combining A208 from murine laminin a1 with the fibronectin active site GRGDS, linked by a glycine spacer. This compound self-assembles into amyloid-like fibrils and facilitates fibroblast cell adhesion through actin stress fiber formation, suggesting its use as a bioadhesive in tissue regeneration and engineering. FN-A208 targets IKVAV receptors and integrins, but its function can be inhibited by EDTA.

Fibronectin is a high-molecular weight (~440kDa) extracellular matrix glycoprotein that binds to membrane-spanning receptor proteins called integrins.In addition to integrins, fibronectin also binds extracellular matrix components such as collagen, fibrin

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

RGD-Targeted Proapoptotic Peptide is a peptide that preferentially binds to integrins at sites of tumor angiogenesis through its C-terminal RGD-4C sequence (ACDCRGDCFC).

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.

SF1126 is a relevant pan and dual first-in-class PI3K/BRD4 inhibitor. SF1126 is an RGDS-conjugated LY294002 prodrug, which is designed to exhibit increased solubility and bind to specific integrins within the tumor compartment.

cRGDfK-thioacetyl ester, a bioactive polypeptide, exhibits selective affinity for integrins and can modify near-infrared (NIR) fluorescent probes for targeted cancer imaging [1] [2].

BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 hydrate selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 hydrate results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels[1][2]. The combination of BIO5192 hydrate (1 mg/kg; i.v.) and Plerixafor (5 mg/kg; s.c.) exert an additive effect on progenitor mobilization[1].BIO5192 hydrate (30 mg/kg; s.c; bid; during days 5 through 14) delays paralysis associated with EAE (experimental autoimmune encephalomyelitis)[2].BIO5192 hydrate (1 mg/kg, i.v.) shows the terminal half-life is 1.1 hours. BIO5192 hydrate (3, 10, and 30 mg/kg; s.c.) shows half-lives of 1.7, 2.7, and 4.7 hours, respectively. The blood plasma curves show that the AUC for the s.c. route of administration increased about 2.5-fold from 5,460 h*ng/ml for the 3 mg/kg dose to 14,175 h*ng/ml for the 30 mg/kg[1]. Animal Model: C57BL/6J x 129Sv/J F1 mice[1] [1]. Ramirez P, et al. BIO5192, a small molecule inhibitor of VLA-4, mobilizes hematopoietic stem and progenitor cells. Blood. 2009;114(7):1340‐1343. [2]. Leone DR, et al. An assessment of the mechanistic differences between two integrin alpha 4 beta 1 inhibitors, the monoclonal antibody TA-2 and the small molecule BIO5192, in rat experimental autoimmune encephalomyelitis. J Pharmacol Exp Ther. 2003;305(3):1150-1162.

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.

GRGDSPK TFA (EMD 56574 TFA) is a peptide containing the Arg-Gly-Asp (RGD) sequence. It acts as a competitive and reversible inhibitor of integrin-fibronectin binding. This compound is utilized in research to elucidate integrins' involvement in bone formation and resorption [1] [2].

Bexotegrast (PLN-74809) is an orally active and potent inhibitor of αvβ6 and αvβ1 integrins with antifibrotic effects, inhibits αvβ6 and αvβ1-induced activation of TGF-β, and can be used for the study of idiopathic pulmonary fibrosis (IPF) and non-specific interstitial pneumonia (NSIP).

Etrolizumab (rhuMAb Beta7), a gut-selective anti-β7 integrin monoclonal antibody, targets the β7 subunit of α4β7 and αEβ7 integrins specifically, demonstrating affinity with K i values of 18 nM for Human α4β7 and 1800 pM for Human αEβ7-293. It is utilized in the research of inflammatory bowel disease (IBD) [1] [2].

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.

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.

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

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.

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

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].

RGD (RGD (Arg-Gly-Asp) Peptides) (Arg-Gly-Asp) Peptides is a cell adhesion motif which can mimic cell adhesion proteins and bind to integrins.

RGD Trifluoroacetate is a tripeptide that effectively triggers cell adhesion, addresses certain cell lines and elicits specific cell responses; RGD Trifluoroacetate binds to integrins.RGD Trifluoroacetate is the most effective and most often employed pept

Integrin modulator 1 is a potent and selective α4β1 integrin agonist, with an IC50 of 9.8 nM for RGD-binding α4β1. Integrin modulator 1 increases cell adhesion mediated by α4β1 integrin, with an EC50 of 12.9 nM[1]. Integrin modulator 1 (2-10 μg/mL; 30 min) significantly increases Jurkat E6.1 cell adhesion[1].Integrin modulator 1 (1-100 nM; 1 h) strongly and significantly increases ERK1/2 phosphorylation in Jurkat E6.1 cells[1].Integrin modulator 1 (1 nM-10 μM; 30 min) significantly increases the binding of HUTS-21 antibody to Jurkat E6.1 cells in a concentration-dependent manner[1]. [1]. Baiula M, et, al. New β-Lactam Derivatives Modulate Cell Adhesion and Signaling Mediated by RGD-Binding and Leukocyte Integrins. J Med Chem. 2016 Nov 10;59(21):9721-9742.

Echistatin TFA, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1[1][2][3][4]. [1]. J Musial, et al. Inhibition of platelet adhesion to surfaces of extracorporeal circuits by disintegrins. RGD-containing peptides from viper venoms. Circulation. 1990 Jul;82(1):261-73.[2]. M Sato, et al. Echistatin is a potent inhibitor of bone resorption in culture. J Cell Biol. 1990 Oct;111(4):1713-23.[3]. C C Kumar, et al. Biochemical characterization of the binding of echistatin to integrin alphavbeta3 receptor. J Pharmacol Exp Ther. 1997 Nov;283(2):843-53.[4]. I Wierzbicka-Patynowski, et al. Structural requirements of echistatin for the recognition of alpha(v)beta(3) and alpha(5)beta(1) integrins. J Biol Chem. 1999 Dec 31;274(53):37809-14.

CWHM-12 is a potent inhibitor of αV integrins (IC50s of 0.2/0.8/1.5/1.8 nM for αvβ8/αvβ3/αvβ6/αvβ1).

Potent irreversible αVβ3 integrin antagonist (Ki = 0.27 nM). Disrupts attachment of osteoclasts to bone and inhibits bone reabsorption (IC50 = 0.1 nM). Prevents ADP-induced platelet aggregation via inhibition of glycoprotein IIb/IIIa (GpIIb/IIIa, αIIbβ3)