l2100 targetmol anticancer libraries  (TargetMol)

Journal: bioRxiv

Article Title: Acquired resistance to the PRMT5 inhibitor confers collateral sensitivity to MEK inhibition in MTAP-null non-small cell lung cancer

doi: 10.64898/2026.04.16.719008

Figure Lengend Snippet: High-throughput drug screen and MEK inhibitor sensitivity in MRTX1719-resistant NSCLC cells. (A) Composition of the compound library used for drug screen, including SGC epigenetic compounds, FDA-approved oncology drugs, and TargetMol epigenetic inhibitors. (B) IC50 values of MRTX1719 and anisomycin in DMSO and MRTXR cells. Anisomycin was included as a nonselective control in the drug screen. (C) Dose-response curves of DMSO and MRTXR cells treated with the MEK inhibitor selumetinib. Data are presented as mean ± SD. (D) Synergy heatmaps of MRTX1719 and selumetinib in DMSO and MRTXR cells. Synergy mean scores were calculated using the Bliss model with the SynergyFinder+ tool.

Article Snippet: The screening library comprised 619 compounds, including SGC epigenetic compounds, TargetMol epigenetic inhibitors, and FDA-approved oncology drugs ( ).

Techniques: High Throughput Screening Assay, Drug discovery, Control

Journal: bioRxiv

Article Title: Acquired resistance to the PRMT5 inhibitor confers collateral sensitivity to MEK inhibition in MTAP-null non-small cell lung cancer

doi: 10.64898/2026.04.16.719008

Figure Lengend Snippet: High-throughput drug screen and MEK inhibitor sensitivity in MRTX1719-resistant NSCLC cells. (A) Composition of the compound library used for drug screen, including SGC epigenetic compounds, FDA-approved oncology drugs, and TargetMol epigenetic inhibitors. (B) IC50 values of MRTX1719 and anisomycin in DMSO and MRTXR cells. Anisomycin was included as a nonselective control in the drug screen. (C) Dose-response curves of DMSO and MRTXR cells treated with the MEK inhibitor selumetinib. Data are presented as mean ± SD. (D) Synergy heatmaps of MRTX1719 and selumetinib in DMSO and MRTXR cells. Synergy mean scores were calculated using the Bliss model with the SynergyFinder+ tool.

Article Snippet: A high-throughput drug screen was performed using a compound library consisting of 619 compounds, including 59 SGC epigenetic compounds, 380 TargetMol epigenetic inhibitors and 180 FDA-approved oncology drugs.

Techniques: High Throughput Screening Assay, Drug discovery, Control

Journal: Acta Neuropathologica Communications

Article Title: Tumor-like proliferation of CCM3 knockout endothelial cells: insights from semaxinib treatment and transcriptome profiling of co-cultures

doi: 10.1186/s40478-026-02283-1

Figure Lengend Snippet: Screening of a cytokine inhibitor library in co-cultures of CCM3 KO and WT iECs. A Scheme of the library screening approach (Created in BioRender. Pilz, R. (2026) https://BioRender.com/lhhhtxj ). B Scheme of the image and data analysis strategy (Created in BioRender. Pilz, R. (2026) https://BioRender.com/o4wswi1 ). The Operetta CLS High-Content Imaging System was used to calculate the total number of nuclei, to allocate the cells to red or green fluorescence (colored outlines of the cells), and to quantify the percentage of green cells of the total cell count per well. The total cell count was used to exclude cytotoxic compounds. Then, statistical analysis was performed to identify hits. C Example of the readout strategy. The first two panels show fluorescence imaging of mEGFP (labeled cytoplasm of AICS-0036 cells), mTagRFP-T (labeled plasma membrane of AICS-0054 cells), and Hoechst 33342 (nuclei) (scale bar = 500 μm). The two panels on the right illustrate the software’s detection and allocation strategy, with an enlarged section for clarity. Nuclei of AICS-0036 cells are outlined in green, while nuclei of AICS-0054 cells are outlined in red. D Representative illustrations of the high-content imaging of plates from one experimental run. The library (compounds) was tested in co-cultures of CCM3 KO (mEGFP) and WT (mTagRFP-T) iECs. DMSO-treated AICS-0036 CCM3 KO/AICS-0054 WT and AICS-0036 WT/AICS-0054 WT co-cultures were used as controls (two columns on the right). E Results of the compound screening showing the percentage of green KO cells from the total cell count for each compound (bars) after excluding cytotoxic compounds. Data are presented as means and SD ( n = 4). All conditions that showed a proportion of green KO cells higher or lower than 50% (purple lines) of the DMSO-treated KO/WT control (highlighted in red) are highlighted in blue. Statistical analysis was performed using one-way ANOVA with Dunnett’s correction (* = Padj < 0.05; *** = Padj < 0.001). All compound-treated conditions were compared against the DMSO-treated control

Article Snippet: The TargetMol cytokine inhibitor library (#L3600, TargetMol Chemicals Inc., Boston, MA, USA; status 2022) was added two hours after seeding at a final concentration of 10 μM per well.

Techniques: Library Screening, Imaging, Fluorescence, Cell Characterization, Labeling, Clinical Proteomics, Membrane, Control