Hdm2 E3 Ligase Inhibitor II, HLI373

A cell-permeable pyrimidoquinoline-dione compound that promotes cellular p53 and E3 ubiquitin ligase HDM2/MDM2 built-ups (optimal conc. = 5 µM in human retinal pigment epithelial RPE cells) via direct inhibition of MDM2-mediated p53 ubiquitination and MDM2 autoubiquitination, resulting in an upregulation of p53-dependent transcription activity (2.5-fold of basal in U2OS-based reporter assays; 5 µM 20 h treatment). Shown to induce apoptotic cell death in E1A-transformed, but not non-transformed, RPE cells (72% death; 10 µM 26 h treatment) and be more active toward wild-type p53-expressing than mutant p53-expressing cancer cells (≥67% vs. ≤37% death induction, respectively; 25 µM 30 h treatment).

A cell-permeable pyrimidoquinoline-dione compound that upregulates cellular p53 and E3 ubiquitin ligase HDM2/MDM2 protein levels (optimal conc. = 5 µM in RPE cells) by directly inhibiting MDM2 E3 ubiquitin ligase activity. Shown to induce apoptotic cell death in E1A-transformed, but not non-transformed, RPE cells and be more active toward wild-type p53-expressing than mutant p53-expressing cancer cells (≥67% vs. ≤37% death induction, respectively; 25 µM 30 h treatment).

Packaged under inert gas

Toxicity: Regulatory Review (Z)

Kitagaki, J., et al. 2008. Mol. Cancer Ther.7, 2445.
Yang, Y., et al. 2005. Cancer Cell7, 547.

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