-
-
Overview
-
Please contact us at for specific academic pricing.
Background
HDM201, also known as Siremadlin or NVP-HDM201, inhibits the Mdm2-p53 protein-protein interaction, with affinity constant for Mdm2 in the picomolar range and a selectivity ratio greater than 10000-fold vs. Mdm4. It binds to the p53 binding-site of the Mdm2 protein, disrupting the interaction of the Mdm2 and p53 proteins as well as leading to the activation of the p53 pathway. Currently, interfering the interaction between the tumor suppressor p53 and its main negative regulator MDM2 has become a therapeutic concept explored to treat cancers.
1. Stachyra-Valat T, Baysang F, D’Alessandro AC, et al. Abstract 1239: NVP-HDM201: Biochemical and biophysical profile of a novel highly potent and selective PPI inhibitor of p53-Mdm2. Cancer Research, 2016, 76(14 Suppl): Abstract nr 1239.
2. Jeay S, Ferretti S, Holzer P, et al. Dose and Schedule Determine Distinct Molecular Mechanisms Underlying the Efficacy of the p53-MDM2 Inhibitor HDM201. Cancer Research, 2018, 78(21): 6257-6267.
-
- Properties
-
Overview