SB-273005 is a potent nonpeptide and orally active integrin antagonist with Kis of 1.2 nM and 0.3 nM for αvβ3 receptor and αvβ5 receptor, respectively[1].
Pinatuzumab is a CD22 monoclonal antibody. Pinatuzumab targets the cell-surface antigen CD22. Pinatuzumab can be used for synthesis of antibody drug conjugates (ADCs) to research several diseases including non-Hodgkin lymphoma (NHL)[1][2].
Tirofiban-d9 is deuterium labeled Tirofiban.
Sibrafiban (RO 48-3657) is the orally active, nonpeptide, double-prodrug of Ro 44-3888 and a selective glycoprotein IIb/IIIa receptor antagonist. Sibrafiban inhibits platelet aggregation[1][2][3].
Chrysotobibenzyl can be isolated from stem of Dendrobium pulchellum. Chrysotobibenzyl inhibits lung cancer cell (H460 and H292) migration, invasion, filopodia formation via Cav-1, integrins β1, β3, and αν, and EMT suppressions. Chrysotobibenzyl also sensitizes lung cancer cell death mediated by Cisplatin (HY-17394)[1].
Arg-Gly-Asp-Ser is an integrin binding sequence that inhibits integrin receptor function, decreases systemic inflammation via inhibition of collagen-triggered activation of leukocytes and attenuates expression of inflammatory cytokines, iNOS and MMP-9.
Odulimomab (anti-LFA1) is an anti-LFA-1 monoclonal antibody. Odulimomab inhibits proliferation of T lymphocyte and shows protective effects against ischemia and reperfusion injury. Odulimomab can be used for the research of transplant rejection and immunological disease[1][2].
SF0166 is a topically administered αvβ3 integrin antagonist, inhibits integrin-ligand interactions with IC50 of 0.6 nM to 13 nM for human αvβ3, αvβ6, and αvβ8; inhibits cellular adhesion to vitronectin across human, rat, rabbit, and dog cell lines with IC50 of 7.6 pM-76 nM; significantly decreases neovascularization in the oxygen-induced retinopathy mouse models. Other Indication Phase 2 Clinical
Echistatin, 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].
Mumefural is a bioactive component of the processed fruit of Prunus mume Sieb. Mumefural inhibits platelet aggregation. Mumefural shows anti-thrombotic effects and ameliorates cognitive impairment[1][2].
Fradafiban is a nonpeptide platelet glycoprotein IIb/IIIa antagonist, which binds to the human platelet GP IIb/IIIa complex with a Kd value of 148 nM.
Irigenin is a is a lead compound, and mediates its anti-metastatic effect by specifically and selectively blocking α9β1 and α4β1 integrins binding sites on C-C loop of Extra Domain A (EDA). Irigenin shows anti-cancer properties. It sensitizes TRAIL-induced apoptosis via enhancing pro-apoptotic molecules in gastric cancer cells[1].
BIO5192 is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 selectively binds to α4β1 (IC50=1.8 μM) 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[1][2].
Etaracizumab (LM 609) is an αvβ3 integrin IgG1 monoclonal antibody. Etaracizumab inhibits angiogenesis and melanoma tumor growth. Etaracizumab can be used to research anticancer[1].
K34c is a potent and selective α5β1 integrin antagonist. K34c can be used for glioblastoma research[1].
ATL 1102 is a novel second-generation antisense oligonucleotide to CD49d mRNA
α2β1 Integrin Ligand Peptide interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors[1].
αvβ1 integrin-IN-2 (compound 32) is a potent inhibitor of integrins ανβ1 and α5β1 with IC50s of 0.9 nM，and 33 nM，respectively. αvβ1 integrin-IN-2 also inhibits other integrins with ，，IC50s of 380 nM (ανβ3)，280 nM (ανβ5)，230 nM (ανβ6)，87 nM (ανβ8)，respectively，in SPRA assay[1].
FITC-Ahx Gly Arg Gly Asp Ser Pro is a GRGDSP (HY-P0290) coupled to FITC. GRGDSP is an integrin inhibitor that can inhibit the adherence of tumor cells to endothelial cells of blood vessels and limit its metastasis[1].
Zalunfiban (RUC-4) acetate is a potent, selective platelet αIIbβ3antagonist (IC50=45 nM). Zalunfiban acetate can be used for the research of myocardial infarction (MI)[1].
A novel specific glycomimetic E-Selectin antagonist with Kd of 0.46 uM, IC50 of 1.75 uM; weakly inhibits L-selectin (IC50=2.9 uM) and >10 uM for P-selectin; not only mobilizes AML cells out of protective niches but also blocks NF-kB activation and prevents this E-selectin-mediated chemoresistance, thereby enhancing the therapeutic effects of standard chemotherapy; also overcomes MM metastasis and chemoresistance. Blood Cancer Phase 2 Clinical
PLN-1474 (compound 1) is an orally active and selective avß1 integrin inhibitor with an IC50 value of ＜50 nM. PLN-1474 reduces levels of pSMAD3/SMAD3 in liver, hepatic collagen gene expression and hepatic OHP concentration in liver fibrosis mouse model. PLN-1474 can be used for the research of preventing, delaying or treating a fibrotic or cirrhotic disease or disorder[1].
Abrilumab is a fully human monoclonal antibody directed against α4β7. Abrilumab selectively binds the α4β7 integrin heterodimer. Abrilumab can be used for the research of inflammatory bowel disease (IBD)[1].
Tirofiban-d9 (L700462-d9) hydrochloride is the deuterium labeled Tirofiban. Tirofiban(L700462) is a potent non-peptide, glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) antagonist[1][2].
Carotegrast is an orally available α4 integrin receptor inhibitor with anti-inflammatories activities.
RO0270608, the active metabolite of R411, is a dual alpha4beta1-alpha4beta7 (α4β1/α4β7) integrin antagonist. Antiinflammatory activity[1][2].
3-Hydroxyxanthone (3-Hydroxy-xanthen-9-one) is a xanthone compound, with . 3-Hydroxyxanthone inhibits NADPH-catalysed lipid peroxidation in human umbilical vein endothelial cells (HUVECs). 3-Hydroxyxanthone also inhibits TNF-alpha induced ICAM-1 expression[1].
XVA143, an α/β I-like allosteric antagonist, inhibits LFA-1 dependent firm adhesion, while at the same time it enhances adhesion in shear flow and rolling both in vitro and in vivo[1].
Cyclo(RGDyK) trifluoroacetate is a potent and selective αVβ3 integrin inhibitor with an IC50 of 20 nM.
Cilengitide is a potent and selective integrin inhibitor for αvβ3 and αvβ5 receptor, with IC50s of 4 and 79 nM, respectively.