Journal: International Journal of Biological Sciences

Article Title: Ebastine exerts antitumor activity and induces autophagy by activating AMPK/ULK1 signaling in an IPMK-dependent manner in osteosarcoma

doi: 10.7150/ijbs.69541

Figure Lengend Snippet: High-throughput screening generates candidate anti-inflammatory agents for osteosarcoma therapy. ( a ) The composition of this immunology inflammation screening library (L4100). ( b-d ) The inhibition rate of every compound in all three osteosarcoma cell lines. ( e ) The inhibition rate > 95% in three osteosarcoma cell lines was achieved by ebastine.

Article Snippet: The immunology inflammation screening library (L4100), dorsomorphin (S7840) and 3-methyladenine (3-MA, S2767) were purchased from Selleck (Shanghai, China).

Techniques: High Throughput Screening Assay, Inhibition

Journal: The Journal of general virology

Article Title: Influenza virus entry via the GM3 ganglioside-mediated platelet-derived growth factor receptor β signalling pathway.

doi: 10.1099/jgv.0.001235

Figure Lengend Snippet: Fig. 4. Virus entry and inhibition by Ki8751 in CHO-wt, CHO-K1, and transfectant cells carrying FGFR4 or VEGFR2. (a) Nuclear import of vRNP in CHO cells incubated with influenza (A/PR/8/34) virus over 1 h at 35 C. Quantitative confocal microscopy was carried out after dual nuclear staining for viral NP and DAPI. In three separate experiments, three images (each containing ~120 cells) were taken from each condition to quantify the green fluorescent signal in the nucleus. (b) Virus binding efficiency relative to CHO-wt cells, as determined by RT-qPCR quantification of cell-bound virus after 60 min of incubation at 4 C. (c) Ki8751 and two other RTK inhibitors, crenolanib and imatinib (all at 60 µM), inhibit virus nuclear entry in CHO-wt and CHO-K1 cells. Confocal microscopy after NP-immunos- taining at 1 h p.i. Green: viral NP; blue: nuclear DAPI staining. (d) vRNA synthesis at 10 h p.i., assessed by two-step RT-qPCR. The y-axis shows the fold increase in vRNA, relative to untreated CHO-wt cells. Panels a, b and d: mean±SEM (N=3). Statistical significance by two- sided Student’s t-test: *P<0.05; ***P<0.005; NS=not significant (P>0.05).

Article Snippet: The library of 276 protein kinase inhibitors was purchased from Selleck Chemicals (catalogue no. L1200).

Techniques: Virus, Inhibition, Transfection, Incubation, Confocal Microscopy, Staining, Binding Assay, Quantitative RT-PCR

Journal: Scientific Reports

Article Title: Identification of novel PAD2 inhibitors using pharmacophore-based virtual screening, molecular docking, and MD simulation studies

doi: 10.1038/s41598-024-78330-5

Figure Lengend Snippet: Graphical summary of the study on PAD2 inhibitor discovery. This figure highlights the stepwise approach, including pharmacophore-based virtual screening, molecular docking, molecular dynamics simulations, and binding energy calculations, leading to the identification of PAD2 inhibitors.

Article Snippet: In the exploration of the covalent inhibitors tools, Cresset’s Flare 5.0 was utilized for docking against 843 compounds from Selleckchem’s covalent library.

Techniques: Binding Assay

Journal: Nature Communications

Article Title: A phenopushing platform to identify compounds that alleviate acute hypoxic stress by fast-tracking cellular adaptation

doi: 10.1038/s41467-025-57754-1

Figure Lengend Snippet: a Overview of AH-to-CH phenopushing screening and hit-calling framework. N: Normoxia. AH: Acute hypoxia (1 d). CH: Chronic hypoxia (6 d). D: Distance from the phenotypic profile of a perturbation (a given compound at a given dose) to the centroid of the phenotypic profiles of CH DMSO controls. θ : Angle of deviation from the phenotypic profile of a perturbation relative to the centroid of the phenotypic profiles of CH DMSO controls. The cell icons: Created in BioRender. Wu, A. (2025) https://BioRender.com/q85j552 . b Summary of geometric hit calls in the primary screen. Scatter plot and density map for distance (x-axis) and direction (y-axis) of bioactive compounds. Red solid line and dotted line show cutoffs for distance and angle, respectively. Vehicle (DMSO) controls in N, AH, and CH are shown for reference. Bioactive non-hit compounds (black dots), hits (red dots), and four hit examples (large red dots) are shown. c Screening funnel for AH-to-CH phenopushing hits. d Representative images for DMSO under N, AH, or CH compared to hit examples (highlighted in b) in AH (Temsirolimus, Deforolimus, KU-0063794, WYE-354). The experiment was independently repeated three times with similar results. Source data are provided as a Source Data file.

Article Snippet: Screened compounds included (1) Selleck FDA-approved & Passed Phase I Drug Library (L3800), (2) Selleck Kinase Inhibitor Library (L1200), (3) Selleck Apoptosis Compound Library (L3300), (4) Selleck Epigenetics Compound Library (L1900), (5) Selleck Bioactive Library (L1700), (6) manually curated FDA-approved & Passed Phase I drugs from other vendors, and (7) manually curated bioactive compounds from other vendors.

Techniques:

Journal: Nature Communications

Article Title: A phenopushing platform to identify compounds that alleviate acute hypoxic stress by fast-tracking cellular adaptation

doi: 10.1038/s41467-025-57754-1

Figure Lengend Snippet: a Overview of the ischemia rescue assay. The cell icons: Created in BioRender. Wu, A. (2025) https://BioRender.com/q85j552 . b Scatter plot of hit compound effects on HepG2 survival in ischemia-like stress. Cell survival: normalized to DMSO-treated cells, averaged across all tested well replicates and doses for each drug, and ranked based on their survival rate. Dashed lines: survival of DMSO-treated hypoxia naïve cells (bottom) or DMSO-treated cells pre-exposed to hypoxia for 6 days (top). mTOR/PI3Ki: AH-to-CH phenopushing hits targeting mTOR and/or PI3Ks. BETi: AH-to-CH phenopushing hits targeting BET proteins. Other: AH-to-CH phenopushing hits other than mTOR/PI3Ki and BET proteins. c Normalized cell survival of each tested dose for the top 25 hits shown in b . d Ischemia rescue effect comparison between the most effective tested dose of phenopushing (red) and non-phenopushing, bioactive (blue) compounds. Kernel density estimation used to smooth histograms. Dashed lines: (grey) mean survival of DMSO-treated cells or (red) 3x DMSO survival. Source data are provided as a Source Data file.

Article Snippet: Screened compounds included (1) Selleck FDA-approved & Passed Phase I Drug Library (L3800), (2) Selleck Kinase Inhibitor Library (L1200), (3) Selleck Apoptosis Compound Library (L3300), (4) Selleck Epigenetics Compound Library (L1900), (5) Selleck Bioactive Library (L1700), (6) manually curated FDA-approved & Passed Phase I drugs from other vendors, and (7) manually curated bioactive compounds from other vendors.

Techniques: Rescue Assay, Comparison