Hdm-2 (human double minute-2; Mdm-2 in mouse) is a ubiquitin ligase and key negative regulator of p53, targeting it for proteasomal degradation. Overexpression of Hdm-2 in some tumors leads to inactivation of p53, thereby allowing tumor cells to escape p53-induced apoptosis.¹ HLI 373 is an inhibitor of Hdm-2.² At concentrations of 5-50 µM, it selectively inhibits autoubiquitylation of Hdm-2 as well as the ubiquitylation and degradation of p53.² Through these actions, HLI 373 stabilizes p53 and increases p53-dependent transcription, inducing apoptosis of transformed cells, tumor cells, and mouse embryo fibroblasts harboring wild-type p53.²

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1.Chène, P. Inhibiting the p53-MDM2 interaction: An important target for cancer therapy. Nature Reviews.Cancer 3, 102-109 (2003).

2.Kitagaki, J.,Agama, K.K.,Pommier, Y., et al. Targeting tumor cells expressing p53 with a water-soluble inhibitor of Hdm2. Molecular Cancer Therapeutics 7(8), 2445-2454 (2015).