ubiquitination related chemical compound library  (TargetMol)

Journal: bioRxiv

Article Title: Phenotypic Screening Identifies Flunarizine as an Inhibitor of Radiotherapy-Induced Astrocyte Reactivity with Therapeutic Potential in Glioblastoma

doi: 10.1101/2025.07.12.664538

Figure Lengend Snippet: (A) Flowchart describing the workflow used to identify compounds that inhibit IR-induced astrocyte reactivity in primary human astrocytes. (B) Jitter plot showing the results of the primary screens, represented as distance scores to the non-IR control for two primary human astrocyte batches and three compound libraries. The dashed line indicates the hit threshold. (C) Pie charts showing the frequency of hits across the three libraries and the distribution of therapeutic classes among hits from the FDA-approved Prestwick Chemicals library. (D) Schematic illustrating the origin of compounds and the experimental strategy used for the confirmation screening. (E) Jitter plot of confirmation screen results represented as distance score to the non-IR control across four primary human astrocyte batches. The dashed line represents the hit threshold. (F) Summary of confirmed hits categorized by compound origin, clinical testing, blood–brain barrier (BBB) permeability, therapeutic class, and molecular targets. The final 12 prioritized compounds are listed.

Article Snippet: On the second day, cells were treated with one of the following libraries: 176 compounds from Enzo SCREEN-WELL Protease, Kinase and Epigenetics (PKE) Inhibitor libraries, 330 compounds from the TargetMol Anti-Cancer drugs library (#L2110, v2018) or 1,280 compounds from the FDA-approved Prestwick Chemical library (prestwickchemical.com, v2016).

Techniques: Control, Permeability

Journal: NPJ Precision Oncology

Article Title: Lestaurtinib’s antineoplastic activity converges on JAK/STAT signaling to inhibit treatment naïve and therapy resistant forms ovarian cancer

doi: 10.1038/s41698-025-00947-0

Figure Lengend Snippet: a Viability of indicated cell lines following 48 h of treatment with 1 µM of the 145 compounds contained in the Cayman Chemical epigenetic drug library (#11076) relative to DMSO vehicle. N = 2. b Drug screen hit prioritization schema. Figure created with BioRender.com. c Dose response curves (two-fold dilution starting at 2.5 µM) and IC50 concentrations for lestaurtinib in a panel of therapy-sensitive and -resistant ovarian cancer cell lines following 5–10 days of treatment. N = 8. Graphs represent mean ± standard error. Abbreviations: Cis Res cisplatin-resistant, Olap R olaparib-resistant.

Article Snippet: Fig. 1 Identification of lestaurtinib as a novel inhibitor of therapy-sensitive and -resistant ovarian cancer cells. a Viability of indicated cell lines following 48 h of treatment with 1 μM of the 145 compounds contained in the Cayman Chemical epigenetic drug library (#11076) relative to DMSO vehicle.

Techniques: Drug discovery