integrin α5β1 inhibitor  (MedChemExpress)

Journal: Bioactive Materials

Article Title: Mechanically sensitized hydrogel microspheres trigger membrane receptor switch for cartilage repair

doi: 10.1016/j.bioactmat.2026.03.017

Figure Lengend Snippet: Integrin receptor activation induced by membrane receptor switch. A) The fluorescence microscopy of MSCs loaded on HAMA or OBNC hydrogel after different treatments. B) Relative fluorescence intensity in the whole field of view for each group. C) Relative fluorescence intensity per cell for each group (∗ symbol represents comparison with HAMA group, # symbol represents comparison with OBNC group). D) Flow cytometry was used to detect integrin αvβ1 and α5β1 positive cells. E) Relative fluorescence intensity of each group. F) Flow cytometry was used to detect 12G10 positive cells and within integrin αvβ1 and α5β1 positive cells. G) Relative fluorescence intensity of each group, and relative proportions of 12G10 to integrins αvβ1 and α5β1. (ns: non-significant, ∗ P < 0.05, ∗∗ P < 0.01, ∗∗∗ P < 0.001, ## P < 0.01, ### P < 0.001).

Article Snippet: TRPC1 inhibitor (0.3 nM, Pico145, CAS No. 1628287-16-0), TRPM7 inhibitor (1.0 μM, VPC4, CAS No. 945604-76-2), TRPV2 inhibitor (5.0 μM, compound IV2-1, CAS No. 2242724-49-6), TRPM4 inhibitor (1.5 μM, CBA, CAS No. 351424-20-9), PIEZO1 inhibitor (2.5 μM, GsMTx4, CAS No. 1209500-46-8), integrin αvβ5 inhibitor (8.0 nM, Compound 12, CAS No.: 2615912-33-7), integrin αvβ1 inhibitor (0.3 nM, Compound C8, CAS No. 1689540-62-2), integrin α5β1 inhibitor (10 μM, ATN-161, 904763-27-5), and CDK5 inhibitor (5 nM, CDK5-IN-1, 2,639,540-19-3) were purchased from MCE Biotechnology Co., LTD. After the MSCs were treated, the cRGD solution was added at a concentration of 1:200 and incubated in the dark for 15 min, and the results were observed by fluorescence microscopy.

Techniques: Activation Assay, Membrane, Fluorescence, Microscopy, Comparison, Flow Cytometry

Journal: bioRxiv

Article Title: Development of Integrin α5β1-targeted PET/NIR imaging probes for glioblastoma intraoperative navigation and intracavity targeted radionuclide therapy

doi: 10.64898/2026.01.09.698741

Figure Lengend Snippet: (A) Strategies for modification of GS, including amino acid mutation, covalent modification, cyclization, and multivalency. (B) SPR sensorgrams demonstrating the binding affinity of GS and GR for human integrin α5β1 in a concentration-dependent manner. The equilibrium dissociation constant (K D ) of each peptide was calculated based on SPR measurements. The K D values of each precursor are shown. (C) Molecular docking of GR and GS binding integrin a5b1 protein (grey; PDB: 7NWL) showing the selected possible ligation residues. (D-F) Analysis of integrin α5β1 expression in U87MG cells and tumor tissues by western blot ( D ), and immunohistochemistry ( E-F ) analysis. The band for integrin α5 was approximately 150 kDa. M, marker. C, cell. T, tumor. For immunofluorescence images, green is for integrin α5, red for integrin β1, and blue for nucleus. Scale bar, 50□μm ( E-F ). (G) In vitro cellular uptake of [ 68 Ga]GS and [ 68 Ga]GR in U87MG cell lines. All results are expressed as means ± SEM, as indicated in at least three independent experiments. “*” represents differences compared with the [ 68 Ga]GS. * p < 0.05.

Article Snippet: Recombinant human integrin α5β1 (alpha 5 beta 1, HY-P77718, MCE, NJ, USA) was immobilized on a CM5 sensor chip at 25 □ following a standard amine coupling kit.

Techniques: Modification, Mutagenesis, Binding Assay, Concentration Assay, Ligation, Expressing, Western Blot, Immunohistochemistry, Marker, Immunofluorescence, In Vitro

Journal: bioRxiv

Article Title: Development of Integrin α5β1-targeted PET/NIR imaging probes for glioblastoma intraoperative navigation and intracavity targeted radionuclide therapy

doi: 10.64898/2026.01.09.698741

Figure Lengend Snippet: (A) Immunofluorescence images show the expression of integrin α5β1, GFAP, and NEUN of U87MG tumors in orthotopic glioblastoma tumor-bearing mice. Green indicates integrin α5, Red for NEUN, yellow for GFAP, and blue for nucleus. Scale bar, 1 mm. (B-C) Representative fluorescence imaging of mice bearing in orthotopic U87MG tumors ( B ) and ex vivo brains ( C ). Cy5-GS and Cy5-GR were intravenously injected with a dose of 5 mg/kg. (D) Quantification of fluorescence intensity in tumors corresponding to ( C ). (E) Immunohistochemical analysis of integrin α5β1 expression in brain tissue sections from orthotopic glioblastoma tumor-bearing mice. Scale bar, 1 mm. (F-G) Immunofluorescence images of brain tissue sections from orthotopic glioblastoma tumor-bearing mice treated with Cy5-GS ( F ) and Cy5-GR ( G ). Green indicates integrin α5, Red for GS or GR, and blue for nucleus. Scale bar, 1 mm. (H-I) Magnific imaging of brain tissue sections from orthotopic glioblastoma tumor-bearing mice treated with GS-Cy5. Scale bar, 50 μm. All results are expressed as means ± SEM, as indicated in at least three independent experiments. A multiple t-test was used when two groups were compared. The symbol “*” represents differences compared with the Cy5-GS. *** p < 0.001.

Article Snippet: Recombinant human integrin α5β1 (alpha 5 beta 1, HY-P77718, MCE, NJ, USA) was immobilized on a CM5 sensor chip at 25 □ following a standard amine coupling kit.

Techniques: Immunofluorescence, Expressing, Fluorescence, Imaging, Ex Vivo, Injection, Immunohistochemical staining

Journal: Journal of Inflammation Research

Article Title: The eNAMPT-Integrin α5β1 Axis Mediates Neutrophil-Endothelial Cell Interactions Driving Inflammation in Ulcerative Colitis

doi: 10.2147/JIR.S554975

Figure Lengend Snippet: Inhibition of integrin α5β1 receptor function attenuates inflammatory injury in DSS-induced colitis in mice. (A ) Body weight of each group was monitored for 10 days (n = 6). ( B ) Representative images of colon and colon length were measured in each group on day 10 (n = 6). ( C ) Representative H&E stained micrographs of colon in each group and quantitative assessment of colon injury using histopathology scores (n = 6); black arrowheads indicate inflammatory cell infiltration (scale bar: 25 μm; original. ( D ) Representative immunohistochemical staining of integrin α5β1 + cells in colonic mucosa (scale bar: 25 μm; original magnification ×400) and quantification of integrin α5β1 + cells per high-power field (n = 6), with black arrows indicating positive cells. ( E ) ELISA assay was performed to examine the serum concentrations of pro-inflammatory cytokines CXCL1, IL-6, TNF-α and IL-1β (n = 6). Statistical analysis was performed by one-way ANOVA. ns: not significant; *: p<0.05; ***: p<0.001.

Article Snippet: The groups of DSS-fed mice were: the UC model group; the anti-Ly6G group, which was injected intraperitoneally with anti-Ly6G antibody (1.25 mg/kg, Selleck, USA) every 2 days to deplete neutrophils; the Daporinad group, which was injected intraperitoneally with Daporinad (2.4 mg/kg, MedChemExpres, USA) every day to inhibit NAMPT activity and reduce eNAMPT levels; ATN-161 group, daily intraperitoneal injection of ATN-161 to block integrin α5β1 receptor function (1 mg/kg, MCE).

Techniques: Inhibition, Staining, Histopathology, Immunohistochemical staining, Enzyme-linked Immunosorbent Assay