Natalizumab is a recombinant, humanized monoclonal antibody, binds to α4β1-integrin and blocks its interaction with vascular cell adhesion molecule-1 (VCAM-1). Natalizumab can be used for the treatment of relapsing remitting multiple sclerosis and Crohn's disease. Natalizumab is also the first targeted therapy which blocks an essential mechanism for lymphocyte entry to the CNS and thus prevents acute demyelinating relapses[1].
Volociximab (M200) is a chimeric human/murine IgG4 antibody IIA1 targeting integrin α5β1 (EC50=0.2 nM). Integrin α5β1 is a major fibronectin receptor involved in angiogenesis. Volociximab has antiangiogenic and antitumor activities and inhibits the proliferation of human umbilical vein vascular endothelial cells (HUVECs)[1][2].
GRGDSP, a synthetic linear RGD peptide, is an integrin inhibitor.
Lifitegrast is an integrin lymphocyte function-associated antigen-1 (LFA-1) antagonist; inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM.
A potent, highly selective α4β1 integrin antagonist with Kd of <10 pM; the rate of BIO7662 binding is dependent on the metal ion concentration; directly competes with VCAM-1, CS-1, and BIO1211 for binding to the integrin.
Cyclo(Arg-Gly-Asp-D-Phe-Val) is an integrin αvβ3 inhibitor. Cyclo(Arg-Gly-Asp-D-Phe-Val) has antitumor activity. Cyclo(Arg-Gly-Asp-D-Phe-Val) can be used for the research of acute myeloid leukemia[1].
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), with a Ki of 25.8 nM. BIRT 377 also inhibits the production of IL-2 in vivo. BIRT 377 can be used for researching inflammatory and immune disorders[1].
Zaurategrast ethyl ester sulfate (CDP323 sulfate), the ethyl ester prodrug of CT7758[1], is a α4β1/α4β7 integrin antagonist used for the treatment of inflammatory and autoimmune disorders[2].
Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) is an inhibitor of integrin αvβ3, with antitumor activity.
LDV-FITC, a fluorescent peptide, is a FITC-conjugated LDV peptide (HY-P2267). LDV-FITC binds to the α4β1 integrin with high affinity (Kd: 0.3 nM and 12 nM for binding to U937 cells in the presence and absence of Mn2+ respectively). LDV-FITC can be used to detect α4β1 integrin affinity[1][2].
Bexotegrast is a potent inhibitor of ανβ6 integrin. Bexotegrast can be used for researching fibrosis such as idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP) (extracted from patent WO2020210404A1, compound 5)[1].
Efalizumab is a targeted T cell modulator, and is a humanized monoclonal antibody of CD11a, the α subunit of LFA-1. Efalizumab inhibits T cell activation, cutaneous T cell trafficking, and T cell adhesion to keratinocytes, can be used for plaque psoriasis research[1].
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[1].
Zaurategrast ethyl ester (CDP323), the ethyl ester prodrug of CT7758[1], is a α4β1/α4β7 integrin antagonist used for the treatment of inflammatory and autoimmune disorders[2].
Zaurategrast (CT7758) is a potent and oral-effective α4-integrin inhibitor.
A-286982 is a potent and allosteric LFA-1/ICAM-1 interaction inhibitor with IC50s of 44 nM and 35 nM in an LFA-1/ICAM-1 binding and LFA-1-mediated cellular adhesion assay, respectively[1][2].
Cilengitide is a potent and selective integrin inhibitor for αvβ3 and αvβ5 receptor, with IC50 values of 4 nM and 79 nM, respectively.
αvβ6 integrin inhibitor 2 is a potent ανβ6 integrin inhibitor with an IC50 of 96.5 nM (WO2020081154A1, example 19)[1].
Tirofiban hydrochloride monohydrate is a potent non-peptide, glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) antagonistIC50 value:Target: integrin IIb/IIIa Tirofiban hydrochloride monohydrate blocks platelet aggregation and thrombus formation. Tirofiban is an antithrombotic used in the treatment of unstable angina.Tirofiban, in a concentration-dependent manner reduced platelet aggregation evoked by ADP (IC50 approximately 70 ng/ml), collagen (IC50 approximately 200 ng/ml), and thrombin (IC50 approximately 5,000 ng/ml).
SB-267268 is a selective and nonpeptidic alpha(v)beta3 (αvβ3) and alpha(v)beta5 (αvβ5) integrins antagonist, with Kis of 0.9, 0.5 and 0.7 nM for human αvβ3, monkey αvβ3 and human αvβ5, respectively. SB-267268 inhibits human and mouse αvβ3 with IC50s of 0.68 and 0.29 nM, respectively. SB-267268 reduces angiogenesis and VEGF expression[1].
EILEVPST is a recombinant human fibronectinderived low-molecular-weight peptide fragment. EILEVPST can promote cell type-specific α4 integrin-mediated adhesion. EILEVPST can be used for the research of thrombogenesis[1].
Fibronectin, a glycoprotein (~500 kDa) present in blood as well as in cells, is a biomarker of tissue injury. Fibronectin binds to membrane-spanning receptor proteins called integrins. Fibronectin also binds to other extracellular matrix proteins such as collagen, fibrin, and heparan sulfate proteoglycans[1].
Lys-Gln-Ala-Gly-Asp-Val (KQAGDV) is the six most carboxyl-terminal amino acids in the fibrinogen γ-chain sequence. Lys-Gln-Ala-Gly-Asp-Val is a cell adhesion peptide which is mediated through the α2bβ3 integrin. Lys-Gln-Ala-Gly-Asp-Val is a potent adhesion ligand for smooth muscle cells (SMCs)[1][2].
Tirofiban (L700462) hydrochloride is a Gp IIb/IIIa receptor antagonist of nonpeptide derivative of tyrosine. Tirofiban hydrochloride induces proliferation and migration on endothelial cell by inducing production of VEGF. Tirofiban hydrochloride can significantly reduces myocardial no-reflow and ischemia-reperfusion injury by alleviating myocardial microvascular structural and endothelial dysfunction in the ischemic area[1][2].
Integrin Antagonists 27 is a small molecule integrin αvβ3 antagonist with binding affinity of 18 nM, as s novel anticancer agent. Target: Integrinin vitro: Integrin Antagonists 27 is treated with a panel of cancer cell-lines (breast cancer cell line MDA-MB-435, breast cancer cell lines MCF-7, mouse fibroblast NIH3T3, ovarian cancer cell line HEY, lung cancer cell line NCI-H1975) with all IC50 of >20 uM.
SR121566A is a novel non-peptide Glycoprotein IIb/IIIa (GP IIb-IIIa) antagonist, which can inhibit ADP-, arachidonic acid- and collagen-induced human platelet aggregation with IC50s of 46±7.5, 56±6 and 42±3 nM, respectively.
ATN-161 trifluoroacetate salt is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.
Cyclo(Arg-Gly-Asp-D-Phe-Cys) (Cyclo RGDfC) is a cyclic RGD peptide which has high affinity to αvβ3. Cyclo(Arg-Gly-Asp-D-Phe-Cys) can be used in the research of tumors[1].
iRGD peptide is a 9-amino acid cyclic peptide, triggers tissue penetration of drugs by first binding to av integrins, then proteolytically cleaved in the tumor to produce CRGDK/R to interact with neuropilin-1, and has tumor-targeting and tumor-penetrating properties.
RWJ 50271 is an selective inhibitor of lymphocyte function-associated antigen-1/intercellular adhesion molecule-1(LFA-1/ICAM-1) interaction with an IC50 of 5.0 μM (HL60 cells)[1].