SW044248 distinguishes itself as an unconventional inhibitor of Topoisomerase 1 (Top1), manifesting selective toxicity towards certain non-small cell lung cancer (NSCLC) cell lines without impacting Topoisomerase 2 (Top2). In cell lines sensitive to SW044248, such as HCC4017 and H292, concentrations of 2, 5, and 10 µM swiftly suppress transcription, translation, and DNA synthesis. Conversely, these effects are not observed in cell lines deemed insensitive, namely HBEC30KT and HCC44. At a concentration of 10 µM, SW044248 prompts the activation of the integrated stress response via the GCN2 and PKR kinases. The compound's mechanism of toxicity in HCC4017 cells is attributed to the inhibition of Top1. However, at doses of 5 and 10 µM, SW044248 does not affect the HBEC30KT and HCC44 cell lines, possibly due to the upregulation of p21CDKN1A[1].
体外研究
SW044248 distinguishes itself as an unconventional inhibitor of Topoisomerase 1 (Top1), manifesting selective toxicity towards certain non-small cell lung cancer (NSCLC) cell lines without impacting Topoisomerase 2 (Top2). In cell lines sensitive to SW044248, such as HCC4017 and H292, concentrations of 2, 5, and 10 µM swiftly suppress transcription, translation, and DNA synthesis. Conversely, these effects are not observed in cell lines deemed insensitive, namely HBEC30KT and HCC44. At a concentration of 10 µM, SW044248 prompts the activation of the integrated stress response via the GCN2 and PKR kinases. The compound's mechanism of toxicity in HCC4017 cells is attributed to the inhibition of Top1. However, at doses of 5 and 10 µM, SW044248 does not affect the HBEC30KT and HCC44 cell lines, possibly due to the upregulation of p21CDKN1A[1].
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