Integrin

Tirofiban（MK383） hydrochloride monohydrate is a non-peptide glycoprotein IIb IIIa antagonist.

Roxifiban acetate（DMP 754 acetate） is a potent GP IIb IIIa antagonist that exhibits antiplatelet aggregation activity via immune mediation and can be used in the study of human thrombocytopenia.

Natalizumab used for the treatment of relapsing remitting multiple sclerosis and Crohn's disease.

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.

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.

ATN-161 trifluoroacetate salt (ATN-161 TFA salt) is a novel integrin α5β1 antagonist that inhibits angiogenesis and growth of liver metastases and improves survival in a murine model.

iRGD peptide (c(CRGDKGPDC)) is a 9-amino acid cyclic peptide (sequence: CRGDKGPDC) and a molecular mimicry agent that was originally identified in an in vivo screening of phage display libraries in tumor-bearing mice.

ICAM-1-IN-1 is a potent and selective inhibitor of E-selectin (IC50 = 7 nM) and ICAM-1 (IC50 = 5 nM).

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

Cyclo(-RGDfK) is a potent and selective inhibitor of integrin αvβ3 with IC50 of 0.94 nM. Cyclo specifically targets tumor microvasculature and cancer cells by binding to αvβ3 integrin on the cell surface.

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.

Cyclo(-RGDfK) is a selective αvβ3 integrin inhibitor(IC50 : 0.94 nM).

CWHM-12 is a potent inhibitor of αV integrins, with IC50 values of 0.2, 0.8, 1.5, and 1.8 nM for αvβ8, αvβ3, αvβ6, and αvβ1, respectively.

SB273005 is an orally active and potent nonpeptide integrin αvβ3 antagonist that inhibits αvβ3 and αvβ5 and reduces the production of Th2 cells and the cytokine IL-10 in pregnant mice.

Vedolizumab, a humanized monoclonal antibody, targets the α4β7 integrin for treating Crohn's disease and ulcerative colitis.

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.

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

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

Cucurbitacin B (Cuc B) has profound in vitro and in vivo antiproliferative effects against human pancreatic Y cells. It inhibited AKT signaling activation through up-regulation of PTEN. Cucurbitacin B is an effective inhibitor of HIF-1 and provide new perspectives into the mechanism of its anticancer activity. Cucurbitacin B inhibits proliferation and induces apoptosis via STAT3 pathway inhibition in A549 lung Y cells.

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.

Volociximab (M200) is an IgG4 monoclonal antibody targeting the α5β1 integrin , with antiangiogenic, antitumor and anticancer activity, inhibits the growth of rabbit VX2 tumors and is used to study solid tumors.

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

Bestatin hydrochloride (Ubenimex hydrochloride) is an inhibitor of aminopeptidase N (APN) CD13 and aminopeptidase B.

Cyclo(RADfK) is a selective α(v)β(3) integrin ligand extensively used for research, therapy, and diagnosis of neoangiogenesis. It also serves as a negative control for cyclo(-RGDfK-), the RGD peptide, which modulates cell adhesion and is recognized by several integrin family members.

E7820 (ER68203-00) is an angiogenesis inhibitor by suppressing integrin a2 (a cell adhesion molecule expressed on endothelial cells).

Irigenin mediates its antimetastatic effect by specifically and selectively blocking the α9β1 and α4β1 integrin binding sites on the C-C loop of the Extra Domain A domain. It can sensitize TRAIL-induced apoptosis by enhancing the expression of pro-apoptotic molecules in gastric cancer cells and has anti-cancer effects.

Carvedilol phosphate hemihydrate (BM 14190 phosphate hemihydrate) is the phosphate salt form of carvedilol, a racemic mixture and adrenergic blocking agent with antihypertensive activity and no intrinsic sympathomimetic activity.

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).

P11 acetate is an integrin αvβ3-vitronectin interaction antagonist(IC50 = 2.74 nM).

BIRT-377 is a negative allosteric and orally bioavailable inhibitor of ICAM-1 and LFA-1(Ki = 25.8 nM). BIRT-377 inhibits the production of IL-2 and can be used in studies about inflammatory and immune disorders.

Lifitegrast (SAR 1118) is an antagonist of lymphocyte function-associated antigen-1.

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

Abciximab (C7E3) is a mouse human chimeric monoclonal antibody that is a potent glycoprotein IIb IIIa inhibitor. Abciximab has anti-platelet aggregation and leukocyte adhesion, acting by binding to glycoproteins IIb IIIa, vitronectin and Mac-1 receptors.

Leukadherin-1 is an allosteric activator of CD11b CD18. Increasing CD11b CD18-dependent cell adhesion to fibrinogen, Decreasing leukocyte motility and transendothelial migration; reduces inflammation.

RWJ 50271 is a selective lymphocyte function-associated antigen-1/intercellular adhesion molecule-1(LFA-1/ICAM-1) interaction inhibitor( IC50 of 5.0 μM in HL60 cells).

Cyclo(RGDyK) trifluoroacetate is a potent and selective αVβ3 integrin inhibitor with an IC50 of 20 nM.

OSU-T315 (OSU-T315 (1,5-regioisomer)) (1,5-regioisomer) is a ILK inhibitor.

LXW7 is an octamer disulfide cyclic peptide and αvβ3 integrin ligand, acts as a potent and specific endothelial progenitor cells (EPCs) and endothelial cells (ECs) targeting ligand. LXW7 is a disulfide cyclic octa-peptide (cGRGDdvc) containing unnatural amino acids flanking both sides of the main functional motif.

Vaccarin is a major flavonoid glycoside in Vaccariae semen, its biotransformation pathways involves methylation, hydroxylation, glycosylation and deglycosylation.

Lifitegrast sodium (SAR-1118-023 sodium) is a small molecule integrin antagonist that inhibits T cell-mediated inflammation by blocking the binding of two important cell surface proteins (lymphocyte function-associated antigen 1 and intercellular adhesion molecule 1), which reduces inflammation of the ocular surface, and may be used in the study of dry eye.

Arginine-glycine-aspartic acid

Tirofiban (L700462) (MK-383) is a selective palate GPIIb IIIa antagonist which inhibits platelet aggregation with IC50 of 9 nM.

A-205804 is a specific and effective inhibitor of E-selectin( IC50=20 nM ) and ICAM-1(IC50=25 nM) expression.

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.

ILK-IN-2 (OSU-T315) is a novel potent, orally active ILK (integrin-linked kinase) inhibitor with IC50 of 0.6 μM.

ILK-IN-3 is an inhibitor of integrin linked kinase, and with antitumor activity.

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

Arg-Gly-Asp-Ser acetate is an integrin binding sequence that directly and specifically bind pro-caspase-8, pro-caspase-9 and pro-caspase-3, while it does not bind pro-caspase-1. Arg-Gly-Asp-Ser acetate inhibits integrin receptor function.