Journal: eLife

Article Title: A drug repurposing approach reveals targetable epigenetic pathways in Plasmodium vivax hypnozoites

doi: 10.7554/eLife.98221

Figure Lengend Snippet: ( A ) Index chart of an epigenetic inhibitor library screened against P. vivax hypnozoites in a v3 (12-day 1-aminobenzotriazole [1-ABT]) assay. Teal circle: library, black square: DMSO, pink triangle: 200 nM nigericin. (B) Structures of epigenetic inhibitor hits which were confirmed to be active against P. vivax hypnozoites in dose–response assays; blue: histone deacetylase inhibitors.

Article Snippet: The Epigenetic Inhibitor library (Targetmol, cat L1200), containing 773 compounds at 10 mM, was purchased and re-plated in pintool-ready 384-well source plates with 200 μM nigericin and DMSO control wells.

Techniques: Histone Deacetylase Assay

Journal: Cell Death & Disease

Article Title: (+)-JQ-1 alleviates cardiac injury in myocardial infarction by inhibiting ferroptosis through the NAMPT/SIRT1 pathway

doi: 10.1038/s41419-025-07880-x

Figure Lengend Snippet: A Screening strategy for small molecular from epigenetic compounds library in H9C2 cardiomyocytes. B Scatter plot of the effect of small molecule compounds in the library on erastin-induced cellular viability in H9C2 cardiomyocytes. Green dots [Log 2 (Fold change) > 4] indicate anti-ferroptosis candidate compounds, blue dots [Log 2 (Fold change) < 0] indicate pro-ferroptosis candidate compounds, gray dots [0≦Log 2 (Fold change) ≦4] indicate compounds that have no effect on ferroptosis. C Effect of JQ-1 (1 μM) on the cell viability in H9C2 cardiomyocytes (up) and neonatal rat ventricular myocytes (NRVMs, down) treated with erastin (2.5 μM). The positive control was represented by the use of Fer-1 (2 μM) (n = 5–6). D The representative images of bright field (BF), Calcein-AM, and propidium iodide (PI) staining in H9C2 cardiomyocytes treated with JQ-1 under the erastin challenge. Green indicates the fluorescence of Calcein-AM, red indicates the fluorescence of PI. Scale bars, 100 µm, (n = 6). E The relative mRNA levels of Ptgs2 and Homx1 in JQ-1-treated H9C2 cardiomyocytes under the erastin challenge (n = 4). F Western blot analysis was conducted to assess the expression of FPN, SLC7A11, and GPX4 in JQ-1-treated H9C2 cardiomyocytes under the erastin challenge. G The relative protein levels of FPN, SLC7A11, and GPX4 were quantified in ( F ) (n = 4). The data are presented as mean ± SEM. The statistical significance of the data was evaluated using a two-way ANOVA followed by Tukey’s test for multiple comparisons ( C , E , and G ). * P < 0.05; ** P < 0.01.

Article Snippet: Subsequently, a total of 773 compounds, belonging to the epigenetic compound library (L1200; TargetMol, USA), were added to the cell culture medium at a final concentration of 5 μM using the Explorer G3 Automated Drug Screening System (PerkinElmer, USA).

Techniques: Positive Control, Staining, Fluorescence, Western Blot, Expressing

Journal: Science Advances

Article Title: BRD4770 protects against DOX-induced cardiotoxicity by inhibiting apoptosis and ferroptosis

doi: 10.1126/sciadv.adw1720

Figure Lengend Snippet: ( A ) Schematic of cell-based high-throughput screening of epigenetic compounds for protection against DOX/erastin-induced cardiomyocyte death. ( B ) The scatter plot of the effect of epigenetic compounds on DOX (top)– or erastin (bottom)–induced cardiomyocyte death. ( C ) Venn analysis of a drug compound. The top 25 compounds that protect against DOX- or erastin-induced cardiomyocyte death were selected separately, overlapping a total of 8 compounds. ( D ) The eight compounds that protect against both DOX- and erastin-induced cardiomyocyte death. Red indicates compounds that have been studied, and green indicates compounds that have not yet been reported in DIC. BDNF, brain-derived neurotrophic factor; JNK1, c-Jun N-terminal kinase 1; TrkA, tropomyosin receptor kinase A; Pim1, proviral integration site for Moloney murine leukemia virus-1 (Pim1) kinase; EGFR, epidermal growth factor receptor; PKA, cAMP-dependent protein kinase; PKC, protein kinase C; HDAC1, histone deacetylase 1. ( E ) The effects of J147 (5 μM), BRD4770 (5 μM), SCR7 pyrazine (5 μM), SMI-4a (5 μM), daphnetin (5 μM), BG45 (5 μM), and entinostat (5 μM) on cell viability in H9C2 cells after 24 hours of DOX or erastin treatment ( n = 6). Statistical significance was determined using (E) one-way analysis of variance (ANOVA) with Tukey’s multiple comparisons. * P < 0.05 and ** P < 0.01.

Article Snippet: After cell adherence, 773 compounds from the Epigenetics Compound Library (L1200, TargetMol, USA) were added at a final concentration of 5 μM to the cell culture medium using the Explorer G3 Automated Drug Screening System (PerkinElmer, USA).

Techniques: High Throughput Screening Assay, Derivative Assay, Virus, Histone Deacetylase Assay