src family inhibitor pp1  (Biomol GmbH)

Journal: Endocrine-Related Cancer

Article Title: Targeting Src tyrosine kinase to enhance radioiodide uptake in breast cancer

doi: 10.1530/ERC-24-0312

Figure Lengend Snippet: Src inhibition inhibits PBF phosphorylation and restores RAIU. (A) MCF-7 (i) and MDA-MB-231 (ii) cells were treated with varying doses of PP1 (0–2 μM) for 24 h before PBF-pY174 and total PBF expression levels were determined by Western blot. (B) Effect of 2 μM PP1 treatment on PBF-mediated RAIU repression in MCF-7 (i) and MDA-MB-231 (ii) cells transiently co-transfected with NIS-MYC. (C) Effect of 2 μM PP1 treatment on PBF-mediated RAIU repression in MCF-7 cells treated with ATRA and dexamethasone. (D) PBF-pY174 and total PBF expression levels following dasatinib dose response (0–2 μM) treatment for 24 h in MCF-7 (i) and MDA-MB-231 (ii) cells. (E) Effect of 1 nM dasatinib or 10 nM saracatinib treatment on PBF-repressed RAIU in MCF-7 (i) and MDA-MB-231 (ii) cells transiently co-transfected with NIS-MYC. n = 3 for all experiments. Error bars = SEM. * = P < 0.05, ** = P < 0.01, *** = P < 0.001.

Article Snippet: Src family kinase inhibitors PP1 (Tocris, UK), dasatinib and saracatinib (Selleck Chemicals, USA) and NMT inhibitor (DDD85646; Drug Discovery Unit, University of Dundee) were dissolved in DMSO to a 10 mM stock concentration.

Techniques: Inhibition, Phospho-proteomics, Expressing, Western Blot, Transfection

Journal: PLoS ONE

Article Title: EGF Receptor Exposed to Oxidative Stress Acquires Abnormal Phosphorylation and Aberrant Activated Conformation That Impairs Canonical Dimerization

doi: 10.1371/journal.pone.0023240

Figure Lengend Snippet: Serum-starved A549 cells were incubated (or not) with 1 µM AG1478 or 5 µM PP1 for 30 min. Then, the cells were treated for 30 min. with 100 ng/ml EGF or 1 U/ml GO, as indicated. EGFR was IPed from cell lysates, resolved by SDS-PAGE and IBed for total receptor, total tyrosine phosphorylation (p-EGFR) and specific Tyr-residue phosphorylation level (Y845, Y1068, Y1086, and Y1173). Protein aliquots of the cell lysates were also directly IBed for total and Y416 phosphorylated (active) c-Src (p-Src).

Article Snippet: PP1, a Src family inhibitor (Enzo Life Sciences), was dissolved in DMSO and added to the treatment medium at a final concentration of 5 µM.

Techniques: Incubation, SDS Page

Journal: PLoS ONE

Article Title: EGF Receptor Exposed to Oxidative Stress Acquires Abnormal Phosphorylation and Aberrant Activated Conformation That Impairs Canonical Dimerization

doi: 10.1371/journal.pone.0023240

Figure Lengend Snippet: A549 cells were incubated (or not) with 5 µM PP1 for 45 min. and then treated (or not) for 15 min. with 100 ng/ml EGF or 30 min. 1 U/ml GO. A . EGFR was IPed from total cell lysates with the mAb 528 and IBed for Y416 phosphorylated c-Src (p-Src) and for total EGFR, as indicated. B . c-Src was IPed from total cell lysates and IBed for total c-Src and EGFR, as indicated.

Article Snippet: PP1, a Src family inhibitor (Enzo Life Sciences), was dissolved in DMSO and added to the treatment medium at a final concentration of 5 µM.

Techniques: Incubation

Journal: Frontiers in Pharmacology

Article Title: Proteasome Inhibition Suppresses KIT-Independent Gastrointestinal Stromal Tumors Via Targeting Hippo/YAP/Cyclin D1 Signaling

doi: 10.3389/fphar.2021.686874

Figure Lengend Snippet: Screening of small molecular inhibitors in KIT-independent GIST62.

Article Snippet: Inhibitors of MEK1/2 (U0126), PI3-K (LY294002), PLCγ (∆609), and JAK (AG490) were from Calbiochem (SanDiego, California) and the Src family inhibitor, PP1, was from Biomol International L.P. (Plymouth Meeting, PA).

Techniques:

Journal: Frontiers in Pharmacology

Article Title: Proteasome Inhibition Suppresses KIT-Independent Gastrointestinal Stromal Tumors Via Targeting Hippo/YAP/Cyclin D1 Signaling

doi: 10.3389/fphar.2021.686874

Figure Lengend Snippet: (A) Cell growth was evaluated in KIT-independent GIST cell line ( GIST62) after treatment with Imatinib (1 μM), PP1 (1 μM), AG490 (10 μM), Δ609 (1 μM), LY294002 (50 μM), U0126 (10 μM), Everolimus (1 μM), Nutlin-3 (5 μM), Bortezomib (100 nM), and 17-AAG (0.5 μM) for 72 h. (B) Immunoblotting evaluated expression of cyclin D1, p53, and p21 in GIST62 cells after treatment with the bortezomib for 72 h. Actin stain is a loading control. Linear capture quantitation of immunoblotting chemiluminescence signals, using an ImageQuant LAS4000. Intensity values are standardized to the DMSO control.

Article Snippet: Inhibitors of MEK1/2 (U0126), PI3-K (LY294002), PLCγ (∆609), and JAK (AG490) were from Calbiochem (SanDiego, California) and the Src family inhibitor, PP1, was from Biomol International L.P. (Plymouth Meeting, PA).

Techniques: Western Blot, Expressing, Staining, Control, Quantitation Assay