Journal: Oncotarget

Article Title: A high-content EMT screen identifies multiple receptor tyrosine kinase inhibitors with activity on TGFβ receptor

doi: 10.18632/oncotarget.8418

Figure Lengend Snippet: Active compounds blocking EMT

Article Snippet: Defined compounds used for validation experiments were ordered de novo from various suppliers: SB-431542, PD-173074, U0126, Salinomycin, Nigericin, PD-161570, PD-166285, PD-166866, Idoxuridine and 5-Azacytidine (all from Sigma); Y-27632 2HCl, GSK429286A, Nintedanib, Pazopanib, Sorafenib, Vatalanib, Axitinib, Sunitinib, Erlotinib, Lapatinib, Gefitinib, Dasatinib, Crizotinib, Vandetanib, AEE788, Cediranib, AZD4547, CP673451, TSU-68 and KX2-391 (all from Selleck Chemicals); PP1, PP2, Rho kinase inhibitor V, SR-3677, GSK269962, SB-772077B (all from Tocris); Fasudil from Enamine; CAY10622 and PD-166326 from Cayman; BGJ398 from Axon Medchem; 5-Aza-2′-deoxycytidine from Chem-Impex.

Techniques: Blocking Assay

Journal: Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie

Article Title: Glucagon-like peptide-1 attenuates endothelial barrier injury in diabetes via cAMP/PKA mediated down-regulation of MLC phosphorylation.

doi: 10.1016/j.biopha.2019.108667

Figure Lengend Snippet: Fig. 3. Changes of endothelial monolayer permeability and F-actin distribution in endothelial cells. (A) Measurement of transendothelial resistance (TER) in en- dothelial cells treated with different concentrations of AGE-BSA, GLP-1 or related signal pathways inhibitors and agonists. (B) Measurement of permeability coef- ficient for albumin (Pa) in endothelial cells treated with different concentrations of AGE-BSA, GLP-1 or related signal pathways inhibitors and agonists. (C) Distribution of F-actin in the cytoskeleton of endothelial cells treated with AGE-BSA, GLP-1 or related signaling pathways inhibitors and agonists. n = 4 for each group. *denotes significant differences compared with BSA group, *P < 0.01; #denotes significant differences compared with AGE-BSA group, #P < 0.05, ##P < 0.01; $denotes significant differences compared with AGE-BSA + GLP-1 group, $P < 0.01. 1.BSA; 2.GLP-1; 3.AGE-BSA; 4.AGE-BSA + GLP-1; 5.AGE- BSA + Forskolin; 6.AGE-BSA + Fasudil; 7.AGE-BSA + RAGE Ab; 8.AGE-BSA + PD98059; 9.AGE-BSA+ SB203580; 10.AGE-BSA + GLP-1 + Exendin (9-39); 11.AGE-BSA + GLP-1 +SQ22536; 12.AGE-BSA + GLP-1 + H89; 13.AGE-BSA + GLP-1 + PMA; 14.AGE-BSA + GLP-1 + LPA.

Article Snippet: HUVECs were pretreated with GLP-1(7-36) (Sigma, USA, Cat. No. G8147), Anti-RAGE antibody (Abcam, Cambridge, UK, Cat. No. 89911), exendin (9-39) (Sigma, USA, Cat. No. E7269), SQ22536 (Tocris Bioscience, Minneapolis, MN, Cat. No. 1435), Forskolin (Sigma, USA, Cat. No. F3917), H89 (Sigma, USA, Cat. No. 1427), Fasudil (Tocris Bioscience, Minneapolis, MN, Cat. No. 0541), LPA (Sigma, USA, Cat. No. L7260), PD98059 (Sigma, USA, Cat. No. P215), SB203580 (Sigma, USA, Cat. No. S8307) or PMA (Sigma, USA, Cat. No. P1585) for 1 h before incubation with AGE-BSA (BioVision, CA, USA, Cat. No. 2221) at 200mg/l.

Techniques: Permeability, Protein-Protein interactions

Journal: Aging Cell

Article Title: Sevoflurane‐induced overexpression of extrasynaptic α5‐GABA A R via the RhoA/ROCK2 pathway impairs cognitive function in aged mice

doi: 10.1111/acel.14209

Figure Lengend Snippet: Fasudil hydrochloride inhibits the abnormal surface expression of α5‐GABA A R and improves cognitive function. (a) Timeline of experience. (b) Western blot images of ROCK2, radixin, and p‐ERM bands in total protein samples and α5‐GABA A R bands in membrane protein samples ( n = 3 per group). β‐Actin and NKA were used as total protein and membrane protein loading controls, respectively. (c–f) The corresponding densitometry analysis of ROCK2, radixin, and p‐ERM in total protein samples and of α5‐GABA A R in surface protein samples (normalized to β‐actin or NKA) ( n = 3). (g) Escape latency in the training stage ( n = 10). (h, i) Swimming speed and time spent in the target quadrant during the probe test ( n = 10). (j) Representative traces of the four groups in the Morris water maze. The escape latency (g) was analyzed with two‐way ANOVA followed by Tukey's multiple comparisons test. All other data were analyzed with one‐way ANOVA followed by Tukey's multiple comparisons test. The data are presented as the mean ± SEM. * p < 0.05, ** p < 0.01, *** p < 0.001; # p < 0.05, ## p < 0.01, ### p < 0.001. IF, immunofluorescence; MWM, Morris water maze; p‐ERM, phosphorylated form of radixin; WB, Western blot.

Article Snippet: To inhibit ROCK2, fasudil hydrochloride (MedChemExpress, NJ, USA) was administered intraperitoneally at a dose of 20 mg/kg/day for 7 days before anesthesia (Zhu et al., ).

Techniques: Expressing, Western Blot, Membrane, Immunofluorescence

Journal: Pharmaceutics

Article Title: Exploring the Ocular Absorption Pathway of Fasudil Hydrochloride towards Developing a Nanoparticulate Formulation with Improved Performance

doi: 10.3390/pharmaceutics16010112

Figure Lengend Snippet: Chemical structure of Fasudil hydrochloride.

Article Snippet: Fasudil hydrochloride was obtained from Biosynth Ltd., Compton, UK.

Techniques:

Journal: Pharmaceutics

Article Title: Exploring the Ocular Absorption Pathway of Fasudil Hydrochloride towards Developing a Nanoparticulate Formulation with Improved Performance

doi: 10.3390/pharmaceutics16010112

Figure Lengend Snippet: Ex vivo permeation study of Fasudil from Fasudil simple solution through excised bovine cornea and sclera for 6 h. Results are expressed (n = 3 ± SD), t -test was performed.

Article Snippet: Fasudil hydrochloride was obtained from Biosynth Ltd., Compton, UK.

Techniques: Ex Vivo

Journal: Pharmaceutics

Article Title: Exploring the Ocular Absorption Pathway of Fasudil Hydrochloride towards Developing a Nanoparticulate Formulation with Improved Performance

doi: 10.3390/pharmaceutics16010112

Figure Lengend Snippet: Flux, apparent permeability coefficient (Papp), lag time (tL), and regression coefficient (R 2 ) of Fasudil simple solution through cornea and sclera.

Article Snippet: Fasudil hydrochloride was obtained from Biosynth Ltd., Compton, UK.

Techniques: Permeability

Journal: Pharmaceutics

Article Title: Exploring the Ocular Absorption Pathway of Fasudil Hydrochloride towards Developing a Nanoparticulate Formulation with Improved Performance

doi: 10.3390/pharmaceutics16010112

Figure Lengend Snippet: Scanning electron micrographs of optimized Cs nanoparticles loaded with Fasudil hydrochloride.

Article Snippet: Fasudil hydrochloride was obtained from Biosynth Ltd., Compton, UK.

Techniques:

Journal: Pharmaceutics

Article Title: Exploring the Ocular Absorption Pathway of Fasudil Hydrochloride towards Developing a Nanoparticulate Formulation with Improved Performance

doi: 10.3390/pharmaceutics16010112

Figure Lengend Snippet: Cumulative release of Fasudil loaded into Cs NPs and Fasudil solution (control) in simulated tear fluid (STF). Results are presented as mean ± SD, n = 3.

Article Snippet: Fasudil hydrochloride was obtained from Biosynth Ltd., Compton, UK.

Techniques: Control

Journal: Pharmaceutics

Article Title: Exploring the Ocular Absorption Pathway of Fasudil Hydrochloride towards Developing a Nanoparticulate Formulation with Improved Performance

doi: 10.3390/pharmaceutics16010112

Figure Lengend Snippet: The coefficients of determination (R 2 ) and the release exponent (n) were obtained through model fitting of the release data of Fasudil from the optimized Cs NPs (results represent mean values ± SD, n = 3).

Article Snippet: Fasudil hydrochloride was obtained from Biosynth Ltd., Compton, UK.

Techniques:

Journal: Pharmaceutics

Article Title: Exploring the Ocular Absorption Pathway of Fasudil Hydrochloride towards Developing a Nanoparticulate Formulation with Improved Performance

doi: 10.3390/pharmaceutics16010112

Figure Lengend Snippet: Trans-corneal permeation profiles of Fasudil from Cs NPs and Fasudil solution (mean ± SD, n = 3).

Article Snippet: Fasudil hydrochloride was obtained from Biosynth Ltd., Compton, UK.

Techniques:

Journal: Pharmaceutics

Article Title: Exploring the Ocular Absorption Pathway of Fasudil Hydrochloride towards Developing a Nanoparticulate Formulation with Improved Performance

doi: 10.3390/pharmaceutics16010112

Figure Lengend Snippet: Flux, apparent permeability coefficient (Papp), lag time (tL), and regression coefficient (R 2 ) of Fasudil through cornea from Fasudil simple solution and Fasudil-Cs NPs.

Article Snippet: Fasudil hydrochloride was obtained from Biosynth Ltd., Compton, UK.

Techniques: Permeability