HDM201 R Enantiomer

Description: HDM201 R Enantiomer is the R enantiomer of HDM201 (also called NVP-HDM201, HDM stands for 'human double minute 2 homolog'). HDM201 is an orally bioavailable, highly potent and selective inhibitor of the p53-Mdm2 protein-protein interaction. It has high affinity for Mdm2 in the picomolar range and a selectivity ratio of more than 10000-fold vs Mdm4. HDM201 is currently undergoing phase I clinical trial for cancer treatment. HDM201 inhibits the binding of the HDM2 protein to the transcriptional activation domain of the tumor suppressor protein p53. By preventing this HDM2-p53 protein-protein interaction, the proteosome-mediated enzymatic degradation of p53 is inhibited, which results in the restoration of both p53 signaling and p53-mediated induction of tumor cell apoptosis.

References: Proc Natl Acad Sci U S A. 2017 Mar 21; 114(12):3151-3156; Bioorg Med Chem Lett. 2016 Oct 1; 26(19):4837-4841.

Related CAS#: 1448867-41-1 (racemic mixture)