Drug intelligence / Profile preview

XS-1017

Development stage
Preclinical
Lead developer
Jiangsu Yayao Biotech
Modality
Small Molecules
01

Overview

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.

02

Targets

MDM2 (Mouse double minute 2 homolog)

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