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].
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.
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].
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].
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[1].
Cyclo(RADfK) is a selective α(v)β(3) integrin ligand that has been extensively used for research, therapy, and diagnosis of neoangiogenesis. Sequence: Cyclo(Ala-Asp-Phe-Lys-Arg).
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.
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].
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].
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 Ki 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)[1][2].
E7820 is an angiogenesis inhibitor by suppressing integrin a2, a cell adhesion molecule expressed on endothelial cells.
Certepetide (CEND-1) is a bifunctional cyclic peptide (a.k.a. iRGD). Certepetide is a tumor-penetrating enhancer via RGD motif interaction with alphav-integrins and via activating NRP-1, and transforms the solid tumor microenvironment into a temporary drug conduit. Certepetide accumulates in tumors, and is used in the research of pancreatic cancer and other solid tumors[1][2][3].
Cys-Arg-Gly-Asp-Phe-Pro-Ala-Ser-Ser-Cys (Disulfide bridge:cys1-cys10), a decapeptide containing a cyclic RGD active sequence, is an Integrin αIIbβ3 antagonist that inhibits platelet and Adhesion of proMMP-13[1].
Firategrast is an orally bioavailable α4β1/α4β7 integrin antagonist.
Vedolizumab (anti-α4β7-integrin) is a humanized IgG1 monoclonal antibody that targets the α4β7 integrin for the treatment of ulcerative colitis and Crohn's disease[1][2].
RGD Trifluoroacetate is a tripeptide that effectively triggers cell adhesion, addresses certain cell lines and elicits specific cell responses; binds to integrins.
Cucurbitacin B belongs to a class of highly oxidized tetracyclic triterpenoids; could repress cancer cell progression.IC50 value:Target: anticancer natural compoundin vitro: Cucurbitacin-B inhibited growth and modulated expression of cell-cycle regulators in SHSY5Y cells. At the molecular level, we found that Cucurbitacin-B inhibited AKT signaling activation through up-regulation of PTEN [1]. CuB induced apoptosis of A549 cells in a -concentration-dependent manner, as determined by fluorescence microscopy, flow cytometry and transmission electron microscopy. CuB dose-dependently inhibited lung cancer cell proliferation, with cell cycle inhibition and cyclin B1 downregulation. Apoptosis induced by CuB was shown to be associated with cytochrome c release, B-cell lymphoma 2 downregulation and signal transducer and activator of transcription 3 pathway inhibition [2]. CuB inhibited ITGA6 and ITGB4 (integrin α6 and integrin β4), which are overexpressed in breast cancer. Furthermore, CuB also induced the expression of major ITGB1and ITGB3, which are known to cause integrin-mediated cell death [3]. Cuc B treatment caused DNA double-strand breaks (DSBs) without affecting the signal transducer and activator of transcription 3 (STAT3), the potential molecular target for Cuc B. Cuc B triggers ATM-activated Chk1-Cdc25C-Cdk1, which could be reversed by both ATM siRNA and Chk1 siRNA. Cuc B also triggers ATM-activated p53-14-3-3-σ pathways, which could be reversed by ATM siRNA [4].in vivo: Efficacy of CuB was tested in vivo using two different orthotopic models of breast cancer. MDA-MB-231 and 4T-1 cells were injected orthotopically in the mammary fat pad of female athymic nude mice or BALB/c mice respectively. Our results showed that CuB administration inhibited MDA-MB-231 orthotopic tumors by 55%, and 4T-1 tumors by 40%. The 4T-1 cells represent stage IV breast cancer and form very aggressive tumors [3].
RGD-4C is a arginine-glycine-aspartic acid peptide (ACDCRGDCFC) with integrin binding activity. The Arg-Gly-Asp (RGD) sequence serves as the primary integrin recognition site in extracellular matrix proteins, and peptides containing this sequence can mimic the recognition specificity of the matrix proteins. RGD-4C is a αv-integrin ligand, can conjugate with bioactive molecule to exert antitumor effects in animal models[1][2][3].
GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits αvβ1-integrin with an IC50 of 1.3 nM.
Surfactin is a potent cyclic lipopeptide biosurfactants that mediates flux of mono-and divalent cations, such as calcium, across lipid bilayer membranes. Surfactin can act as an antimicrobial adjuvant with anti-bacterial, anti-fungal, antimycoplasma and hemolytic effects[1][2]. Surfactin also has antiviral activity against a variety of enveloped viruses[3].
Cyclo(Ala-Arg-Gly-Asp-3-aminomethylbenzoyl) is a selective RGD peptide antagonist and has the potential for Pulmonary arterial hypertensionResearch[1].
mP6 (Myr-FEEERA-OH) is a myristoylated peptide. mP6 inhibits the interaction of Gα13 with integrin β3 without disrupting talin-dependent integrin function. mP6 can block the GTP usage of Rac1, Rap1, and Rab7, effectively inhibiting the infection of CHO-A24 cells[1].
Cepeginterferon alfa-2b is a pegylated interferon. And Cepeginterferon alfa-2b has PEG with molecular weight of 20 kDa as a pegylated base. Cepeginterferon alfa-2b can be used for research of various diseases, such as hepatitis C virus (HCV), polycythemia vera (PV) and essential thrombocythemia (ET)[1][2].
BOP sodium is a potent and selective dual α9β1/α4β1 integrin inhibitor with Kd values in the picomolar range. BOP sodium shows the rapid and preferential mobilization of hematopoietic stem cell (HSC) and progenitors. BOP sodium has little inhibitory activity on α4β7, α1β1, α2β1, and α5β1, αIIBβ3 integrins[1][2].
KGDS is synthetic peptides, targeting integrin GPIIb-IIIa located on the membrane of human activated platelets. Amino acid sequence: Lys-Gly-Asp-Ser[1].
TG53 is a potent inhibitor of tissue transglutaminase (TG2) and fibronectin (FN) protein-protein interaction. TG53 inhibits formation of a complex with integrin β1 and activation of FAK and c-Src during SKOV3 cell attachment onto FN. TG53 can be used for ovarian cancer research[1].