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: Advanced Science

Article Title: Intratumoral Collagen Deposition Supports Angiogenesis Suggesting Anti‐angiogenic Therapy in Armored and Cold Tumors

doi: 10.1002/advs.202409147

Figure Lengend Snippet: Collagen upregulates SOX18 expression through the integrin α5β1/MEK/ERK signaling pathway. a) Expression levels of collagen receptors across different cell types in the scRNA‐seq dataset, with ITGB1 and ITGA5 showing the highest positive correlation. b) Spatial charting of ITGA5‐B1 and VWF in the P10_T4 LUAD sample from Marco De Zuani et al.’s study, [ ²⁶ ] alongside ITGA5‐B1 expression in endothelial and non‐endothelial cells in the spatial transcriptomic dataset. Statistical significance was determined using the Chi‐square test. *** P < 0.001. c) Expression levels of SOX18, ITGA5, and ITGB1 in tumor cells (A549 and H1299), HUVECs, and CAFs. d) Enhanced co‐localization of ITGA5 and ITGB1 following collagen stimulation. Scale bar = 5 µm. e) Impact of collagen stimulation and ITGA5‐B1 blockade on the MEK/ERK pathway in HUVEC cells. f) Effects of collagen stimulation and MEK/ERK inhibition on SOX18 expression in HUVEC cells. g) Effects of collagen stimulation, ITGA5‐B1 blockade, and MEK/ERK blockade on the subcellular localization of SOX18 in HUVEC cells. Scale bar = 5 µm. Statistical significance was determined using ANOVA with Tukey's multiple‐comparison test. ns, non‐significance, *** P < 0.001. n = 3 per group. h) Effects of collagen stimulation, ITGA5‐B1 blockade, and MEK/ERK blockade on the expression of SOX18 downstream targets, MMP7 and CXCL12, in HUVEC cells. Statistical significance was determined using ANOVA with Tukey's multiple‐comparison test. ** P < 0.01, *** P < 0.001. n = 3 per group. Abbreviations: ITGB1: integrin beta 1; ITGA5: integrin alpha 5; VWF: von‐Willebrand factor; SOX18: sex determining region Y box 18; CAF: cancer‐associated fibroblast.

Article Snippet: The integrin α5β1 inhibitor, ATN‐161, [ ] was obtained from TargetMol (catalog T10397) at a working concentration of 1 µmol L −1 , and the MAPK inhibitor, U0126, [ ] was purchased from TargetMol (catalog T21332) with a working concentration of 5 µmol L −1 for in vitro assays.

Techniques: Expressing, Inhibition, Comparison

Journal: Advanced science (Weinheim, Baden-Wurttemberg, Germany)

Article Title: Intratumoral Collagen Deposition Supports Angiogenesis Suggesting Anti-angiogenic Therapy in Armored and Cold Tumors.

doi: 10.1002/advs.202409147

Figure Lengend Snippet: Figure 6. Collagen upregulates SOX18 expression through the integrin 𝛼5𝛽1/MEK/ERK signaling pathway. a) Expression levels of collagen receptors across different cell types in the scRNA-seq dataset, with ITGB1 and ITGA5 showing the highest positive correlation. b) Spatial charting of ITGA5-B1 and VWF in the P10_T4 LUAD sample from Marco De Zuani et al.’s study,[26] alongside ITGA5-B1 expression in endothelial and non-endothelial cells in the spatial transcriptomic dataset. Statistical significance was determined using the Chi-square test. ***P < 0.001. c) Expression levels of SOX18, ITGA5, and ITGB1 in tumor cells (A549 and H1299), HUVECs, and CAFs. d) Enhanced co-localization of ITGA5 and ITGB1 following collagen stimulation. Scale bar = 5 μm. e) Impact of collagen stimulation and ITGA5-B1 blockade on the MEK/ERK pathway in HUVEC cells. f) Effects of collagen stimulation and MEK/ERK inhibition on SOX18 expression in HUVEC cells. g) Effects of collagen stimulation, ITGA5-B1 blockade, and MEK/ERK blockade on the subcellular localization of SOX18 in HUVEC cells. Scale bar = 5 μm. Statistical significance was determined using ANOVA with Tukey’s multiple- comparison test. ns, non-significance, ***P < 0.001. n = 3 per group. h) Effects of collagen stimulation, ITGA5-B1 blockade, and MEK/ERK blockade on the expression of SOX18 downstream targets, MMP7 and CXCL12, in HUVEC cells. Statistical significance was determined using ANOVA with Tukey’s multiple-comparison test. **P < 0.01, ***P < 0.001. n = 3 per group. Abbreviations: ITGB1: integrin beta 1; ITGA5: integrin alpha 5; VWF: von-Willebrand factor; SOX18: sex determining region Y box 18; CAF: cancer-associated fibroblast.

Article Snippet: In Vitro Inhibition of SOX18, Integrin α5β1, and MAPK Cascade: The SOX18 inhibitor, Sm4,[92] was purchased from MedChemExpress (Catalog HY-116940), with a working concentration of 10 μmol L−1 for in vitro assays.

Techniques: Expressing, Inhibition, Comparison

Journal: Nature Communications

Article Title: Epidermal growth factor-like domain 7 drives brain lymphatic endothelial cell development through integrin αvβ3

doi: 10.1038/s41467-024-50389-8

Figure Lengend Snippet: a FISH and antibody staining shows ilk is expressed in GFP+ BLECs at 4 dpf (arrowheads). n = 17/18 embryos. b – g Inhibition of ILK by cpd22 can partially rescue the absence of BLECs in the egfl7 mutant at 6 dpf ( b – e ). Quantification of the number of BLECs in the double loops of brain in different treatment groups ( f , n = 10 embryos, two-tailed unpaired t test. Data are represented as mean ± SD). The statistics show the percentage of embryos that have double lymphatic loops, single loops, and none of the loops in the brain ( g , WT, n = 51 embryos, WT + cpd22, n = 67 embryos, egfl7-/- , n = 116 embryos, egfl7-/- + cpd22, n = 127 embryos, χ 2 test).). h – k An egfl7 mutant was crossed with an ilk heterozygote to generate two types of larvae: ilk +/+; egfl7 -/- and ilk +/-; egfl7 -/-, which were then studied for BLECs loop-structures formation. The larvae were classified into three categories based on their phenotype: Double loops, single loops, and none of the loops ( h – j ). The results showed that compared to ilk +/+; egfl7 -/-, the ilk +/-; egfl7 -/- larvae had a decreased percentage of the none of the loops phenotype, and a partially rescued percentage of double loops and single loops phenotype ( k , ilk +/+; egfl7 -/-, n = 49 embryos, ilk +/-; egfl7 -/-, n = 47 embryos, χ2 test). Scale bar, 50 μm.

Article Snippet: The integrin α5β1 inhibitor-ATN-161(Selleck, #262438-43-7) and the integrin αvβ3 inhibitor-Cilengitide (MCE, #HY16141) stock solution of 10 mM in DMSO was used to prepare a working solution-50 μM and treat the embryos from 54 hpf to 5 dpf.

Techniques: Staining, Inhibition, Mutagenesis, Two Tailed Test