Integrin Inhibitor

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.

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.

ICAM-1-IN-1 is a potent and selective inhibitor of E-selectin and ICAM-1 with IC₅₀ values of 7 and 5 nM, respectively.

Obtustatin is a non-RGD disintegrin consisting of 41 residues. Obtustatin inhibits the adhesion of α1β1 integrin to type IV Collagen (HY-NP003), blocks α1β1 integrin signaling in endothelial cells, and suppresses FGF2-induced angiogenesis. Obtustatin inhibits tumor progression in mouse models and upregulates VEGF expression in sarcoma-bearing mice. Obtustatin can be used in research related to Lewis lung carcinoma and S-180 sarcoma.

Isoxanthohumol is an orally active flavonoid compound. Isoxanthohumol has biological activities such as anti-tumor, anti-inflammatory, antioxidant, antiviral, antifungal, and inhibition of adipogenesis. Isoxanthohumol can induce apoptosis, autophagy, and migration of tumor cells. Isoxanthohumol is active against viruses such as HSV, BVDV, CMV, and Rhino. Isoxanthohumol can be used for the research of tumors, metabolic, and inflammatory diseases.

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.

Synstatin (92-119) is an inhibitor of αvβ3/αvβ5 integrins and IGF1R with anti-angiogenic, anti-proliferative, antioxidant and anti-tumor activities. Synstatin (92-119) competitively blocks the capture of αvβ3/αvβ5 integrins and IGF1R by syndecan-1, disrupts the formation of the syndecan-1 : integrin : IGF1R ternary complex, inhibits integrin activation and talin-mediated signaling pathways, and blocks VEGF-induced angiogenesis. Synstatin (92-119) is applicable to research related to cancer and hepatocellular carcinoma.

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.

Obtustatin triacetate is a 41-residue non-RGD disintegrin. Obtustatin triacetate can be isolated from the venom of Vipera lebetina obtusa. Obtustatin triacetate is a potent and selective inhibitor of integrin α1β1 adhesion to type IV collagen. Obtustatin triacetate inhibits angiogenesis and may be used in cancer research.

ST6GAL1-IN-1 is an orally active selective ST6GAL1 inhibitor (IC₅₀ = 20 μM). ST6GAL1-IN-1 exhibits high antimetastatic potential, effectively inhibiting the migration of MDA-MB-231 cells at noncytotoxic concentrations. ST6GAL1-IN-1 can disrupt integrin sialylation in MDA-MB-231 cells. ST6GAL1-IN-1 inhibits tumor angiogenesis and cancer metastasis via the Integrin/VEGFR2-mediated signaling pathway. ST6GAL1-IN-1 effectively suppresses both tumor growth and cancer metastasis on the MDA-MB-231 xenograft model. ST6GAL1-IN-1 can be used for the study of Triple-negative breast cancer (TNBC).

PLN-1474 (compound 1) is an orally active and selective ανβ1 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 researching a fibrotic or cirrhotic disease or disorder.

Intetumumab (CNTO 95) is a human monoclonal antibody targeting αv integrin, with a K_d value of 1-24 nM. Through high-affinity binding to αv integrin, Intetumumab inhibits its interaction with extracellular matrix proteins (such as vitronectin and fibronectin), thereby blocking the downstream focal adhesion kinase signaling pathway. This further inhibits the adhesion, migration and invasion of tumor cells as well as the proliferation of vascular endothelial cells, promotes cell apoptosis, and exerts anti-tumor and anti-angiogenic effects. Intetumumab can be used in research related to head and neck cancer, non-small cell lung cancer and uterine serous papillary carcinoma.

Spirulina C-phycocyanin, a component of the light-harvesting phycobilisome complex in photosystem II, is a highly dominant chromoprotein in Spirulina. Spirulina C-phycocyanin can be detected by Raman spectral measurement. Spirulina C-phycocyanin has antioxidant, anti-inflammatory, antiplatelet, liver-protective and cholesterol-lowering effects.

Bersanlimab (BI-505) is a fully human monoclonal antibody that targets intercellular adhesion molecule-1 (ICAM-1 or CD54). Bersanlimab has anticancer effects.

Levocarnitine propionate hydrochloride (L-Propionylcarnitine chloride) is used to study diseases such as renal function deterioration, congestive heart failure, and intermittent claudication.

Anti-Mouse CD54 Antibody (YN1/1.7.4) is an anti-mouse CD54 IgG2b antibody inhibitor derived from host Rat. Anti-Mouse CD54 Antibody (YN1/1.7.4) can neutralize CD54 also known as Intercellular Adhesion Molecule-1 (ICAM-1). Anti-Mouse CD54 Antibody (YN1/1.7.4) can be used for the research of inflammation.