par1 antagonist sch79797  (Tocris)

Journal: CytoJournal

Article Title: A disintegrin-like and metalloproteinase 15 facilitates glioblastoma proliferation and metastasis through activation of the protease-activated receptor 1

doi: 10.25259/Cytojournal_92_2024

Figure Lengend Snippet: Inhibition of ADAM15-induced proliferation, migration, and invasion by PAR-1 antagonist treatment. (a) Evaluation by scratch assay after PAR-1 antagonist SCH79797 or PAR-2 antagonist FSLLRY-NH2 treatment. Scale bar = 100 μm. Objective: 100×. (b) Relative migration rate for scratch assay after PAR-1 antagonist SCH79797 or PAR-2 antagonist FSLLRY-NH2 treatment. (c) Evaluation by transwell assay with Matrigel invasion for 72 h. Scale bar = 50 μm. Objective: 200×. (d) Relative invasion rate for transwell assay after PAR-1 antagonist SCH79797 or PAR-2 antagonist FSLLRY-NH2 treatment. (e) Clonogenic assay in U251 and U87. (f) Measurement of colony number after PAR-1 antagonist SCH79797 or PAR-2 antagonist FSLLRY-NH2 treatment. n = 5 independent replicates. ns: No significant, ✶ ✶ ✶ P < 0.001. ADAM15: A disintegrin-like and metalloproteinase 15, PAR1: Protease-activated receptor 1.

Article Snippet: PAR1 antagonist: SCH79797 (Cat. No: SML1939, Merck Millipore, Billerica, MA, USA).

Techniques: Inhibition, Migration, Wound Healing Assay, Transwell Assay, Clonogenic Assay

Journal: CytoJournal

Article Title: A disintegrin-like and metalloproteinase 15 facilitates glioblastoma proliferation and metastasis through activation of the protease-activated receptor 1

doi: 10.25259/Cytojournal_92_2024

Figure Lengend Snippet: Inhibition of ADAM15-induced EMT by PAR-1 antagonist treatment. (a) Western blotting of E-cadherin, N-cadherin, and Vimentin protein expression after PAR-1 antagonist SCH79797 or PAR-2 antagonist FSLLRY-NH2 treatment in U251. (b) Histogram of E-cadherin, N-cadherin, and Vimentin protein expression in U251. (c) Western blotting of E-cadherin, N-cadherin, and Vimentin protein expression after PAR-1 antagonist SCH79797 or PAR-2 antagonist FSLLRY-NH2 treatment in U87. (d) Histogram of E-cadherin, N-cadherin, and Vimentin protein expression in U87. (e) Immunofluorescence of E-cadherin and Vimentin staining in U251 and U87. Scale bar = 20 μm. Objective: 400×. n = 5 independent replicates. ns: Not significant, ✶ ✶ P < 0.01. ADAM15: A disintegrin-like and metalloproteinase 15, PAR1: Protease-activated receptor 1, Epithelial-mesenchymal transition.

Article Snippet: PAR1 antagonist: SCH79797 (Cat. No: SML1939, Merck Millipore, Billerica, MA, USA).

Techniques: Inhibition, Western Blot, Expressing, Immunofluorescence, Staining

Journal: Chinese Medicine

Article Title: Gastrodin attenuates diabetic cardiomyopathy characterized by myocardial fibrosis by inhibiting the KLK8-PAR1 signaling axis

doi: 10.1186/s13020-024-01035-4

Figure Lengend Snippet: KLK8 exerts biological effects through the activation of the PAR1 receptor, which is involved in HG-PA-induced differentiation, collagen synthesis, and the migration of CFs. A–D OE-KLK8-treated CFs were continuously transfected for 12 h. Interventions were performed using the PAR1 and PAR2 antagonists SCH79797 and FSLLRY-NH2. E-G. The PAR1 antagonist SCH79797 was used to treat HG-PA-exposed CFs. A OE-KLK8-overexpressing CFs were treated with the PAR1 antagonist SCH79797 (10 µM) or the PAR2 antagonist FSLLRY-NH2 (1 µM). The MTT assay was performed to determine the proliferation rate of the cells; *P < 0.05 vs. control; # P < 0.05 vs. OE-KLK8. B Immunoblotting of KLK8 and the fibrosis-associated proteins α-SMA, TGFβ1, Collagen I, and Collagen III. C Immunofluorescence staining of α-SMA (green); the nuclei were restained with DAPI (blue); scale bar = 50 μm. D Wound healing assay; scale bar = 50 μm. E Immunoblotting of KLK8 and the fibrosis-associated proteins α-SMA, TGFβ1, Collagen I, and Collagen III. F Immunofluorescence staining of α-SMA (green). The cell nuclei were restained with DAPI (blue); scale bar = 50 μm. G Wound healing assay; scale bar = 50 μm. The data are expressed as the mean ± SEM of three independent experiments; *p < 0.05, **p < 0.01, ***p < 0.001, and ****p < 0.0001.

Article Snippet: Gastrodin (GAS) (G2129091, purity: ≥98%) was purchased from Shanghai Aladdin Biochemical Technology Co., Ltd. PAR1 (141136–83 − 6, 1:1000), pSmad3 (YT4334, 1:1000), Smad3 (HY-P80325, 1:1000), SCH79797 (HY-14993), FSLLRY-NH2 (HY-P1260), and TFLLR-NH2 (HY-P0226A) were purchased from MedChemExpress.

Techniques: Activation Assay, Migration, Transfection, MTT Assay, Control, Western Blot, Immunofluorescence, Staining, Wound Healing Assay