integrin αvβ1 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: Nature Communications

Article Title: Metabolism archetype cancer cells induce protumor TREM2 + macrophages via oxLDL-mediated metabolic interplay in hepatocellular carcinoma

doi: 10.1038/s41467-025-62132-y

Figure Lengend Snippet: A UMAP of the Scissor-selected cells (left). Barplot shows the distribution of Scissor + cells across different myeloid populations and conditions (right). B Forestplot shows the hazard ratios and 95% confidence intervals for different myeloid cluster signatures and clinical information according to a multivariable Cox model in the TCGA-LIHC cohort ( n = 353 patients). Squares represent the hazard ratios, and the horizontal bars extend from the lower limits to the upper limits of the 95% confidence intervals of the estimates of the hazard ratios. C Dotplot displays the DEGs between Scissor + cells and all other cells. D Dotplot displays the expression correlation of SPP1 with other genes in myeloid cells (left). Heatmap shows the expression correlation of indicated genes with SPP1 in myeloid cells from adjacent non-tumor (ANT) and tumor samples (right). E Representative images and quantification of TREM2, SPP1, and CD68 immunofluorescence staining on human HCC sections. Representative cells that denote the co-upregulation of TREM2 and SPP1 in CD68 + TAMs are circled by a dotted line. Scale bar, 50 μm. F Kaplan–Meier survival analysis of HCC patients from the TCGA-LIHC cohort categorized into groups based on normalized TREM2 and SPP1 expression. The cutpoints for patient grouping were calculated by the surv_cutpoint function from the survminer R package. G Barplot shows the mean expression of SPP1 across different myeloid cell populations (upper) and in TAMs from ICB-R and ICB-NR HCC samples (lower). H Dotplot shows the expression of SPP1 ligands in CD8 + T cells (above) or cancer cells (below) from pre-ICB, ICB-NR, and ICB-R HCC scRNA-seq samples. I Schematic of the interaction between TREM2 + TAMs and CD8 + T cells or cancer cells in immunotherapy-resistant HCC. J Heatmap shows the relative expression of indicated genes in isolated TREM2 + /TREM2 − TAMs. K Flow cytometry of IFNγ expression in CD8 + T cells co-cultured with human HCC-isolated TREM2 - TAMs or TREM2 + TAMs ± SPP1 antibody (1 μg/mL). CD8 + T cells were isolated from human PBMC and then activated with anti-CD3/CD28 + IL-2 (50 U/mL) before co-culture assays. L Violin plots display the expression of IFNG and TNF in CD8 + T cells from ICB-NR or ICB-R scRNA-seq samples, with two-tailed Wilcoxon-test statistics. M Dotplot shows the relative expression of IFNG and TNF in CD8 + T cell clusters. N Tissue preference of CD8 + T cell clusters, revealed by odds ratio (OR) value. O Relative cell viability (mean of n = 3 biological replicates) for Hep3B cells treated with a half-log dilution series of TNF (2.5–250 ng/mL) and IFNγ (1–100 ng/mL), cocultured with human HCC-isolated TREM2 - TAMs or TREM2 + TAMs ± SPP1 antibody (1 μg/mL). P Relative cell viability of Hep3B cells treated with mock, SPP1 (50 ng/mL), integrin inhibitor TFA (100 μM), TNF (250 ng/mL) plus IFNγ (100 ng/mL) (TNF/IFNγ), TNF/IFNγ plus SPP1, or TNF/IFNγ plus SPP1 plus TFA (100 μM) for 24 h. Q Relative cell viability for patient-derived HCC organoid with indicated treatment. Data represent the mean ± SD, n = 5 biological replicates in ( P ), n = 6 biological replicates in ( K , Q ). Statistical significance was determined by two-tailed Wald test ( B ), two-tailed unpaired t test ( K , P , Q ), two-tailed Wilcoxon signed rank test ( L ), and log rank test ( F ). Schematic in I was created in BioRender. Chu, T. (2025) https://BioRender.com/r2v4jgs . Source data are provided as a Source Data file.

Article Snippet: Then, TNF (100 ng/mL) + IFNγ (100 ng/mL) (TNF/IFNγ), TNF/IFNγ plus SPP1 (50 ng/mL) or a combination of TNF/IFNγ, SPP1, and integrin inhibitor TFA (HY-100445A, MCE, 50 μM) was added to the culture medium.

Techniques: Expressing, Immunofluorescence, Staining, Isolation, Flow Cytometry, Cell Culture, Co-Culture Assay, Two Tailed Test, Derivative Assay

Journal: Frontiers in Immunology

Article Title: Thrombospondin-1 mitigates osteoarthritis progression by inhibiting mechanical stress-induced chondrocyte ferroptosis via the integrin/YAP pathway

doi: 10.3389/fimmu.2025.1577234

Figure Lengend Snippet: THBS1 inhibits mechanical stress-induced ferroptosis in chondrocytes through integrinαVβ1. Human chondrocytes were stimulated at 1MPa mechanical stress for 2 hours with or without integrinαVβ1 inhibitor αVβ1 integrin-IN- 1(100ng/ml) and rhTHBS1(100ng/ml). Relevant tests were performed 24 hours after the end of mechanical stress stimulation. (A) The cell death ratio of chondrocytes was tested by cell death/live analysis. Scale bar = 50 μm. (B) The cell number of PI (red fluorescence)/calcein (green fluorescence) reflected the cell death ratio (n=3 for each group). (C) Mitochondrial membrane potential was detected by JC-1 assay. Scale bar = 10 μm. (D) The relative IOD ratio of red fluorescence to green fluorescence was used for quantitative analysis (n=3 for each group). (E) Representative TEM images of chondrocytes of indicated groups. (n=3 for each group). Green arrows show the normal mitochondria. Red arrows show the shrunken mitochondria. Scale bars, 1 μm (low field), 500 nm (high field). (F) Representative fluorescence images of mitochondria in chondrocytes. Scale bar = 50 μm. (G) Quantitative analysis of fluorescence intensity (n=3 for each group). (H) Representative images of ROS levels in chondrocytes. Scale bar = 50 μm. (I) Quantitative analysis of fluorescence intensity (n=3 for each group). (J) The expression of GSH in chondrocytes of indicated groups was detected by ELISA (n=3 for each group). (K) Western blot (WB) analysis of Col2, MMP-9 and GPX4. (L-N) Quantification of WB analysis (n=3 for each group). Data were presented as the mean ± SD. **P<0.01.

Article Snippet: IntegrinαVβ1 inhibitor αVβ1 integrin-IN- 1 was obtained from MCE (HY-145363). αVβ1 integrin-IN- 1(100ng/ml) ( ) was added to chondrocytes at the same time of mechanical stress stimulation with or without rhTHBS1, and incubated for 24 hours after the end of mechanical stress stimulation.

Techniques: Fluorescence, Membrane, Expressing, Enzyme-linked Immunosorbent Assay, Western Blot

Journal: Frontiers in Immunology

Article Title: Thrombospondin-1 mitigates osteoarthritis progression by inhibiting mechanical stress-induced chondrocyte ferroptosis via the integrin/YAP pathway

doi: 10.3389/fimmu.2025.1577234

Figure Lengend Snippet: The interaction between THBS1 and IntegrinαVβ1 is enhanced under mechanical stress. (A) Interaction network of differential genes, each circle represented a gene, and the size of the circle represented the core level of the gene. The larger the circle, the higher the core level the gene had in the network. (B) Cartoon shows various binding domains of THBS1 and its receptors. (C) Representative immunostaining of THBS1 showing colocalization with integrins αv and β1 (white arrows) but not with integrin β3, CD47, or CD36 under mechanical stress (n = 6). Scale bars, 50 μm. (D) Quantification of colocalization of THBS1 with molecules shown in C using Image J software. (E) Immunoprecipitation (IP) with anti-THBS1 or control immunoglobulin G (IgG) followed by Western blotting for integrins αv and β1 (n = 3). IB, immunoblot. Data were presented as the mean ± SD. **P<0.01.

Article Snippet: IntegrinαVβ1 inhibitor αVβ1 integrin-IN- 1 was obtained from MCE (HY-145363). αVβ1 integrin-IN- 1(100ng/ml) ( ) was added to chondrocytes at the same time of mechanical stress stimulation with or without rhTHBS1, and incubated for 24 hours after the end of mechanical stress stimulation.

Techniques: Binding Assay, Immunostaining, Software, Immunoprecipitation, Control, Western Blot

Journal: Frontiers in Immunology

Article Title: Thrombospondin-1 mitigates osteoarthritis progression by inhibiting mechanical stress-induced chondrocyte ferroptosis via the integrin/YAP pathway

doi: 10.3389/fimmu.2025.1577234

Figure Lengend Snippet: THBS1 inhibits mechanical stress-induced ferroptosis in chondrocytes through integrinαVβ1. Human chondrocytes were stimulated at 1MPa mechanical stress for 2 hours with or without integrinαVβ1 inhibitor αVβ1 integrin-IN- 1(100ng/ml) and rhTHBS1(100ng/ml). Relevant tests were performed 24 hours after the end of mechanical stress stimulation. (A) The cell death ratio of chondrocytes was tested by cell death/live analysis. Scale bar = 50 μm. (B) The cell number of PI (red fluorescence)/calcein (green fluorescence) reflected the cell death ratio (n=3 for each group). (C) Mitochondrial membrane potential was detected by JC-1 assay. Scale bar = 10 μm. (D) The relative IOD ratio of red fluorescence to green fluorescence was used for quantitative analysis (n=3 for each group). (E) Representative TEM images of chondrocytes of indicated groups. (n=3 for each group). Green arrows show the normal mitochondria. Red arrows show the shrunken mitochondria. Scale bars, 1 μm (low field), 500 nm (high field). (F) Representative fluorescence images of mitochondria in chondrocytes. Scale bar = 50 μm. (G) Quantitative analysis of fluorescence intensity (n=3 for each group). (H) Representative images of ROS levels in chondrocytes. Scale bar = 50 μm. (I) Quantitative analysis of fluorescence intensity (n=3 for each group). (J) The expression of GSH in chondrocytes of indicated groups was detected by ELISA (n=3 for each group). (K) Western blot (WB) analysis of Col2, MMP-9 and GPX4. (L-N) Quantification of WB analysis (n=3 for each group). Data were presented as the mean ± SD. **P<0.01.

Article Snippet: IntegrinαVβ1 inhibitor αVβ1 integrin-IN- 1 was obtained from MCE (HY-145363). αVβ1 integrin-IN- 1(100ng/ml) ( ) was added to chondrocytes at the same time of mechanical stress stimulation with or without rhTHBS1, and incubated for 24 hours after the end of mechanical stress stimulation.

Techniques: Fluorescence, Membrane, Expressing, Enzyme-linked Immunosorbent Assay, Western Blot

Journal: Frontiers in Immunology

Article Title: Thrombospondin-1 mitigates osteoarthritis progression by inhibiting mechanical stress-induced chondrocyte ferroptosis via the integrin/YAP pathway

doi: 10.3389/fimmu.2025.1577234

Figure Lengend Snippet: THBS1 inhibits chondrocyte ferroptosis through the integrinαVβ1/YAP pathway. THBS1 knockout chondrocytes and normal chondrocytes were subjected to 1 MPa mechanical stress for 2 hours, with or without the addition of YAP1 inhibitor PROTAC YAP d1 (20μM) and rhTHBS1(100ng/ml). Immediately following stimulation, IF detection was performed. Additional analyses were conducted after chondrocytes were further incubated with or without YAP1 inhibitor PROTAC YAP d1 (20μM) and rhTHBS1(100ng/ml) for 24 hours post-stimulation. (A) Representative image of chondrocytes undergoing IF detection immediately after mechanical stress stimulation. YAP (red) and DAPI (blue) are also shown. Scale bar = 20 μm. (B) Quantification of YAP localization. In each experiment 150 to 200 cells were evaluated (n = 3). YAP localization in the nucleus (green) or cytoplasm (red) is shown. (C) Western blot (WB) analysis of YAP1. (D) Quantification of WB analysis (n=3 for each group). (E) Representative image of chondrocytes undergoing IF detection immediately after mechanical stress stimulation. YAP (red) and DAPI (blue) are also shown. Scale bar = 20 μm. (F) Quantification of YAP localization. In each experiment 150 to 200 cells were evaluated (n = 3). (G) Western blot (WB) analysis of YAP1. (H) Quantification of WB analysis (n=3 for each group). (I) Mitochondrial membrane potential was detected by JC-1 assay. Scale bar = 10 μm. (J) The relative IOD ratio of red fluorescence to green fluorescence was used for quantitative analysis (n=3 for each group). (K) Representative TEM images of chondrocytes of indicated groups. (n=3 for each group). Green arrows show the normal mitochondria. Red arrows show the shrunken mitochondria. Scale bars, 5.0 μm (low field), 500 nm (high field). (L) Representative fluorescence images of mitochondria in chondrocytes. Scale bar = 50 μm. (M) Quantitative analysis of fluorescence intensity (n=3 for each group). (N) The expression of GSH in chondrocytes of indicated groups was detected by ELISA (n=3 for each group). Data were presented as the mean ± SD. NS P>0.05 *P<0.05, **P<0.01.

Article Snippet: IntegrinαVβ1 inhibitor αVβ1 integrin-IN- 1 was obtained from MCE (HY-145363). αVβ1 integrin-IN- 1(100ng/ml) ( ) was added to chondrocytes at the same time of mechanical stress stimulation with or without rhTHBS1, and incubated for 24 hours after the end of mechanical stress stimulation.

Techniques: Knock-Out, Incubation, Western Blot, Membrane, Fluorescence, Expressing, Enzyme-linked Immunosorbent Assay