FIGURE 1 from Discovery and Characterization of ZL-2201, a Potent, Highly Selective, and Orally Bioavailable Small-molecule DNA-PK Inhibitor

• DOI: 10.1158/2767-9764.24073438.v1
• Publication Date: 2023-09-01T18:25:43Z
• Authors: Shruti Lal; Neil E. Bhola; Bee-Chun Sun; Yuping Chen; Tom Huang; Vivian Morton; Kevin X. Chen; Shanghua Xia; Haoyu Zhang; Nehal S. Parikh; Qiuping Ye; O. Petter Veiby; David I. Bellovin; Yuhua Ji

<p>Evaluation of ZL-2201 antiproliferative activity <i>in vitro</i>. <b>A,</b> Chemical structure ZL-2201, a potent and selective DNA-PK inhibitor. <b>B,</b> Concentration-dependent response to in M059J M059K glioblastoma cancer cells measured by CTG after 6-day treatment. The graph represents the average inhibitory (IC<sub>50</sub>) values (<i>n</i> = 3). <b>C,</b> CRISPR KO ATM A549 FaDu 6 days 2–5). <b>D,</b> IC<sub>50</sub> responses mutant cell lines (black bars) versus WT line (gray bar). Cell growth was 2–6). NCI-H1703 (<b>E</b>) (<b>F</b>) were treated with bleomycin (10 μmol/L) for 2 hours followed addition increasing concentration hours. Whole-cell lysates harvested, concentration-dependent inhibition protein analyzed Simple Western.</p>