373226

Hdm2 E3 Ligase Inhibitor II, HLI373

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.

• Synonym(s): 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
• Empirical Formula (Hill Notation): C₁₈H₂₃N₅O₂ · 2HCl
• CAS Number: 502137-98-6
• Molecular Weight: 414.33
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• assay: ≥98% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic); protect from light
• color: cream
• solubility: water: 50 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: O=C1C2=C(NCCCN(C)C)C3=C(C=CC=C3)N(C)C2=NC(N1C)=O.[2HCl]
• InChI: 1S/C18H23N5O2.2ClH/c1-21(2)11-7-10-19-15-12-8-5-6-9-13(12)22(3)16-14(15)17(24)23(4)18(25)20-16;;/h5-6,8-9,19H,7,10-11H2,1-4H3;2*1H
• InChI key: WUEMKAQTAIRDOA-UHFFFAOYSA-N

Description

General description

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).

Packaging

Packaged under inert gas

Warning

Toxicity: Regulatory Review (Z)

Other Notes

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

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable