fak phosphorylation inhibitor defactinib  (MedChemExpress)

Journal: Oncology Research

Article Title: Degradation of FAK-targeting by proteolytic targeting chimera technology to inhibit the metastasis of hepatocellular carcinoma

doi: 10.32604/or.2024.046231

Figure Lengend Snippet: FAK promotes the EMT of HCC. E-cadherin expression was lower, and vimentin expression was higher in liver cancer tissues with high FAK expression compared with paracancer tissues with low FAK expression (* p < 0.05; ** p < 0.01; *** p < 0.001; **** p < 0.0001) (A) Action diagram. FAK phosphorylation inhibitors can inhibit FAK phosphorylation. FAK PROTAC inhibited the kinase-dependent and non-kinase-dependent functions of FAK by degrading FAK. (B) Experimental flow chart (C).

Article Snippet: Defactinic, an FAK phosphorylation inhibitor, was purchased from MedChemExpress [ ] (MCE, Shanghai, China), and FAK PROTAC (FC-11) was produced by MOE Key Laboratory of Protein Sciences, School of Pharmaceutical Sciences, MOE Key Laboratory of Bioorganic Phosphorus Chemistry & Chemical Biology, Tsinghua University.

Techniques: Expressing

Journal: Theranostics

Article Title: An exosomal-carried short periostin isoform induces cardiomyocyte proliferation

doi: 10.7150/thno.57243

Figure Lengend Snippet: CPC-derived Exo induce neonatal cardiomyocyte cycling via periostin-mediated FAK activation. A. Western analysis of focal adhesion kinase (FAK) phosphorylation in neonatal cardiomyocytes treated with naïve CPC-derived Exo (ExoCPC), Exo from CPC transfected with a siRNA against periostin (ExoCPC_SiPOSTN), or PBS (Ctrl). Quantitative analysis of FAK phosphorylation (fold-changes over Ctrl; n = 4; * p =0.0187 and p =0.0220). B. Western analysis of F-actin and G-actin expression. Quantitative analysis of F-actin/G-actin ratio (fold-changes over Ctrl; n = 6; * p =0.0419 and p =0.0172). C. Quantitative analysis of F-actin intensity in cardiac troponin I (cTnI)-positive cells (fold-change over Ctrl; n = 3; * p =0.0356 and p =0.0455). D. Western analysis of the effect of the FAK phosphorylation inhibitor, PF-573228, on FAK phosphorylation. E. Quantitative analysis of the effect of PF-573228 on EdU-positive cardiomyocytes (fold-changes; n = 4 to 5; ** p =0.0064 and p =0.0048). F. Quantitative analysis of the effect of PF-573228 on phosphorylated histone H3 (pH3)-positive cardiomyocytes nuclei (fold changes; n = 4 to 6; ** p =0.0033 and p =0.0068).

Article Snippet: FAK phosphorylation inhibitor, PF-573228 (10 mM; Sigma), was added to cells 30 min before Exo treatment.

Techniques: Derivative Assay, Activation Assay, Western Blot, Transfection, Expressing

Journal: Theranostics

Article Title: An exosomal-carried short periostin isoform induces cardiomyocyte proliferation

doi: 10.7150/thno.57243

Figure Lengend Snippet: CPC-derived Exo induce in vitro and in vivo cardiomyocyte cycling via periostin-mediated YAP nuclear translocation. A. Cultured neonatal rat cardiomyocytes immunostained for YAP (red) and cardiac-specific α-actinin (sarcomeric; green); nuclear staining with DAPI (blue). Scale bars: 200 µm. Quantitative analysis of YAP fluorescence intensity in the nuclear fraction of cardiomyocytes treated with naïve CPC-derived Exo (ExoCPC), Exo from CPC transfected with a siRNA against periostin (ExoCPC_SiPOSTN), or PBS (Ctrl; n = 5; * p =0.0316; ** p =0.0049). B. Western analysis of YAP and histone H3 in the nuclear fraction of cardiomyocytes and PF-573228 pre-treated cardiomyocytes. Quantitative analysis of YAP levels normalized for H3 in the nuclear fraction (fold-changes over Ctrl; n = 4 to 6; * p =0.0240; ** p =0.0052). C. Knocking down of YAP expression in the nuclear fraction using a siRNA against YAP (SiYAP; fold-changes over naive cells; n = 3; *** p =0.0002). D. Quantitative analysis of the effect of SiYAP on EdU-positive cardiomyocytes (fold-changes over the respective controls; n = 4 to 5; ** p =0.0064 and p =0.0048). E. Quantitative analysis of the effect of SiYAP on phosphorylated H3 (pH3)-positive cardiomyocytes (fold-changes over the respective controls; n = 4 to 6; ** p =0.0033 and p =0.0068). F. Western analysis of YAP and H3 levels in dispersed isolated cardiomyocytes at day 14 after IP injection of ExoCPC, ExoCPC_SiPOSTN or PBS. Quantitative analysis of YAP levels normalized for H3 (fold-changes over Ctrl; n = 5; * p =0.0300 and p =0.0258). G. Western analysis of YAP and H3 levels in dispersed isolated cardiomyocytes from adult rat hearts explanted 14 days after MI and intramyocardial injection of ExoCPC, ExoCPC_SiPOSTN, or PBS. Quantitative analysis of YAP levels normalized for H3 (fold- changes over Ctrl; n = 6).

Article Snippet: FAK phosphorylation inhibitor, PF-573228 (10 mM; Sigma), was added to cells 30 min before Exo treatment.

Techniques: Derivative Assay, In Vitro, In Vivo, Translocation Assay, Cell Culture, Staining, Fluorescence, Transfection, Western Blot, Expressing, Isolation, Injection