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XS-1017 is a preclinical small molecule inhibitor developed by Jiangsu Yayao Biotech that targets the interaction between the tumor suppressor protein p53 and its negative regulator, MDM2 (Mouse double minute 2 homolog). By binding to the p53-binding pocket of MDM2, XS-1017 prevents the formation of the p53-MDM2 complex, thereby inhibiting MDM2-mediated ubiquitination and subsequent proteasomal degradation of p53. This stabilization restores p53's transcriptional activity, leading to the induction of cell cycle arrest, DNA repair, and apoptosis in p53-wild-type cancer cells. The compound is being developed for a variety of indications, including hematological malignancies such as acute myeloid leukemia, polycythemia vera, and lymphomas, as well as various solid tumors including melanoma and soft tissue sarcoma.
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