The Hdm2 E3 Ligase Inhibitor II, HLI373, also referenced under CAS 502137-98-6, controls the biological activity of Hdm2 E3 Ligase. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.
別名:
Hdm2 E3 Ligase Inhibitor II, HLI373, 5-(3-Dimethylaminopropylamino)-3,10-dimethyl-10H-pyrimido[4,5-b]quinoline-2,4-dione, 2HCl, MDM2 Inhibitor VI, MDM2 E3 Ligase Inhibitor II
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).
包装
Packaged under inert gas
警告
Toxicity: Regulatory Review (Z)
その他情報
Kitagaki, J., et al. 2008. Mol. Cancer Ther.7, 2445. Yang, Y., et al. 2005. Cancer Cell7, 547.
法的情報
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
The proto-oncogene MDM2 is frequently amplified in many human cancers and its overexpression is clinically associated with a poor prognosis. The oncogenic activity of MDM2 is demonstrated by its negative regulation of tumor suppressor p53 and the substrate proteins involved
