hsp90 inhibitor screening assay kit  (BPS Bioscience)

Journal: Journal of Enzyme Inhibition and Medicinal Chemistry

Article Title: Delivering bioactive cyclic peptides that target Hsp90 as prodrugs

doi: 10.1080/14756366.2019.1580276

Figure Lengend Snippet: Chemical structures of molecules based on LB51 and their corresponding cell permeability and inhibitory activity in protein binding assays. P app represents the cell permeability × 10 −6 cm/s. The graph shows the impact of series II on the Hsp90-Cyp40 interaction, compared to LB51 and DMSO. Experiments were conducted in triplicate and data represents mean ± SEM of at least 2 independent experiments.

Article Snippet: The binding assays were performed using an Hsp90 (C-terminal) Inhibitor Screening Kits (cat. 50314 or 50317) purchased from BPS Bioscience.

Techniques: Permeability, Activity Assay, Protein Binding

Journal: Journal of Enzyme Inhibition and Medicinal Chemistry

Article Title: Delivering bioactive cyclic peptides that target Hsp90 as prodrugs

doi: 10.1080/14756366.2019.1580276

Figure Lengend Snippet: (a) The impact of LB51 and LB63 versus LB51(Ac) 2 –Cbz and LB63(Ac) 2 –Cbz on the Hsp90-Cyp40 interaction. Experiments were conducted in triplicate and data represent mean ± SEM of at least two independent experiments. (b) Competitive assays where LB51-Tag is competing for binding with LB51(Ac) 2 –Cbz, or LB63(Ac) 2 –Cbz to the C-terminal domain of Hsp90. Experiments were conducted in duplicate and data represent mean ± SEM of two independent experiments.

Article Snippet: The binding assays were performed using an Hsp90 (C-terminal) Inhibitor Screening Kits (cat. 50314 or 50317) purchased from BPS Bioscience.

Techniques: Binding Assay

Journal: British Journal of Cancer

Article Title: Antiproliferative and proapoptotic activity of GUT-70 mediated through potent inhibition of Hsp90 in mantle cell lymphoma

doi: 10.1038/sj.bjc.6606007

Figure Lengend Snippet: ( A ) GUT-70 effects on Hsp90 client proteins. MCL cells were treated with GUT-70 (JVM-2, 5 μ M ; Granta 519, 5 μ M ; Jeko-1, 1 μ M ; MINO, 5 μ M ) for indicated times. Cells were subjected to lysis and analysed by western blot. Western blot images are representative results from three independent experiments. ( B ) GUT-70 competitively inhibited geldanamycin binding to the Hsp90 α subunit. The competition of GUT-70 with FITC-labelled geldanamycin for binding to purified recombinant Hsp90 α was measured. Fluorescence was measured at λ ex 485 nm and at λ em 525 nm. Results shown are means±s.d. from three independent experiments. ( C ) GUT-70 induced protein ubiquitination. JVM-2 and MINO cells were treated with 5 μ M GUT-70 for 24 h, subjected to lysis, and immunoblotted for ubiquitin. Representative results are shown from three independent experiments. ( D ) Proteasome inhibitor bortezomib prevented GUT-70-mediated decreased expression of c-Raf. JVM-2 and MINO cells were treated with 5 μ M GUT-70 and/or 10 n M bortezomib for 24 h, subjected to lysis, and immunoblotted for c-Raf. Western blot images are representative results from three independent experiments.

Article Snippet: The Hsp90 α inhibitor screening assay kit with Hsp90 α recombinant enzyme and fluorescein isothiocyanate (FITC)-labelled geldanamycin was used (BPS Bioscience, San Diego, CA, USA).

Techniques: Lysis, Western Blot, Binding Assay, Purification, Recombinant, Fluorescence, Expressing