Integrin Inhibitor

Abciximab (C7E3), a chimeric mouse/human monoclonal antibody fragment, is a glycoprotein (GP) IIb/IIIa inhibitor. Abciximab inhibits platelet aggregation and leucocyte adhesion by binding to the glycoprotein IIb/IIIa, vitronectin and Mac-1 receptors.

Cyclo(RGDyK) is a potent and selective α_Vβ₃ integrin inhibitor with an IC₅₀ of 20 nM.

BIO5192 is a selective and potent integrin α4β1 (VLA-4) inhibitor (K_d<10 pM). BIO5192 selectively binds to α4β1 (IC₅₀=1.8 nM) over a range of other integrins. BIO5192 results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels.

ABH (hydrochloride) is an orally active arginase inhibitor (K_i = 8.5 nM). ABH hydrochloride promotes NO production and reduces the expression of inflammatory response-related molecules (ICAM-1, VCAM-1, MCP-1). ABH hydrochloride improves erectile function, reduces lung damage, promotes wound healing, reduces arterial blood pressure, and improves vascular fibrosis.

OSU-T315 (ILK-IN-1) is a small Integrin-linked kinase (ILK) inhibitor with an IC₅₀ of 0.6 μM, inhibiting PI3K/AKT signaling by dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain). OSU-T315 abrogates AKT activation by impeding AKT localization in lipid rafts and triggers caspase-dependent apoptosis in an ILK-independent manner. OSU-T315 causes cell death through apoptosis and autophagy.

SGN-B6A is an ADC, which targets integrin beta-6 (ITGB6) through human IgG1 monoclonal antibody Sigvotatug (HY-P990764), and exhibits cytotoxicity against multiple integrin beta-6-positive cancer cell through mitotic inhibitor MMAE (HY-15162).

BIRT 377 is a potent amd orally bioavailable inhibitor of the interaction between intercellular adhesion molecule-1 (ICAM-1) and lymphocyte function-associated antigen-1 (LFA-1). BIRT 377 also inhibits the production of IL-2 in vivo. BIRT 377 can be used for researching inflammatory and immune disorders.

Etrolizumab (rhuMAb Beta7) is a gut-selective, anti-β7 integrin monoclonal antibody. Etrolizumab is specific targeting of the β7 subunit of α4β7 and αEβ7 integrins with K_i values of 18 nM and 1800 pM for Human α4β7 and Human αEβ7-293, respectively. Etrolizumab can be used in research of inflammatory bowel disease (IBD).

αvβ1 integrin-IN-1 TFA (Compound C8) is a potent and selective αvβ1 integrin inhibitor with an IC₅₀ of 0.63 nM. Antifibrotic effects.

Cyclo(-RGDfK) TFA is a potent and selective inhibitor of the α_vβ₃ integrin, with an IC₅₀ of 0.94 nM. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface.

Maltotetraose can serve as a substrate for enzyme-linked assays to measure amylase activity in biological fluids. Maltotetraose has oral active, and reduces TNF-α-induced inflammatory responses by inhibiting NF-κB activity and decreasing ICAM-1 expression. Maltotetraose also inhibits PDGF-induced vascular smooth muscle cell migration and neovascularization. Additionally, Maltotetraose derivatives can function as probes for detecting bacterial infections by targeting the maltodextrin transporter. With good long-term safety, Maltotetraose holds promise for research in atherosclerosis-related diseases.

Etaracizumab (LM 609) is an α_vβ₃ integrin IgG mAb. Etaracizumab is developed to target α_vβ₃+ cancer cells via NK cell-mediated cytotoxicity. Etaracizumab sterically hinders access of large ligands to the RGD-binding pocket, without obstructing it. Etaracizumab decreases p-Akt in vitro. Etaracizumab can decrease cancer proliferation and invasion. Etaracizumab induces tumor cell apoptosis, and inhibition ofα_vβ₃-mediated cell adhesion, endothelial cell migration and osteoclast-mediated bone resorption. Etaracizumab can be studied in anti-tumor research against cancers such as ovarian cancer, metastatic melanoma as well as advanced solid tumors. Recommend Isotype Control: Human IgG1 kappa, Isotype Control (HY-P99001).

Gly-Arg-Gly-Asp-Ser (GRGDS) is a pentapeptide that forms the cell-binding domain of a glycoprotein, osteopontin. Gly-Arg-Gly-Asp-Ser binds to integrin receptors αvβ3 and αvβ5 with estimated IC₅₀ of ～5 and ～6.5 μM

Carotegrast (HCA2969) is an orally active α4 integrin inhibitor with anti-inflammatory activity. Carotegrast can be used in the research of inflammation-related diseases, such as ulcerative colitis.

Anti-Mouse LPAM-1/Integrin α4β7 Antibody (DATK32) is a rat-derived anti-LPAM-1/Integrin α4β7 IgG2a, κ type antibody inhibitor. Anti-Mouse LPAM-1/Integrin α4β7 Antibody (DATK32) specifically reacts with both chains of the α4β7 heterodimer and blocks the adhesion to immobilized mucosal addressin cell adhesion molecule-1 (MAdCAM-1). Anti-Mouse LPAM-1/Integrin α4β7 Antibody (DATK32) suppresses the proliferation and cytokine secretion of CD8+ T cells. Anti-Mouse LPAM-1/Integrin α4β7 Antibody (DATK32) decreases Peyer’s patches and follicular B cells in mice. Anti-Mouse LPAM-1/Integrin α4β7 Antibody (DATK32) can be used for the researches of inflammation, such as ulcerative colitis.

GRGDSPK (EMD 56574) is a peptide incluing Arg-Gly-Asp (RGD). GRGDSPK (EMD 56574) is an competitive and reversible inhibitory peptide for inhibiting integrin-fibronectin binding. GRGDSPK is used to study the role of integrins in bone formation and resorption.

Lifitegrast (SAR 1118) sodium is a potent integrin antagonist. Lifitegrast sodium blocks the binding of intercellular adhesion molecule 1 (ICAM-1) to lymphocyte function-associated antigen 1 (LFA-1), interrupting the T cell-mediated inflammatory cycle. Lifitegrast sodium inhibits Jurkat T cell attachment to ICAM-1 with an IC₅₀ of 2.98 nM. Lifitegrast sodium can be used for researching dry eye disease.

RGD peptide (GRGDNP) TFA is an inhibitor of integrin-ligand interactions. RGD peptide (GRGDNP) TFA competitively inhibits α5β1 binding with extracellular matrice (ECM). RGD peptide (GRGDNP) TFA promotes apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing. RGD peptide (GRGDNP) TFA plays an important role in cell adhesion, migration, growth, and differentiation.

αvβ1 integrin-IN-1 (Compound C8) is a potent and selective αvβ1 integrin inhibitor with an IC₅₀ of 0.63 nM. Antifibrotic effects.

Abituzumab (DI17E6) is a humanised anti-integrin αV monoclonal antibody (IgG2 type). Abituzumab effectively reduces the phosphorylation of FAK, Akt and ERK. Abituzumab can be used in cancer research, particularly in prostate cancer.