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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

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About This Item

Empirical Formula (Hill Notation):
C18H23N5O2 · 2HCl
CAS Number:
502137-98-6
Molecular Weight:
414.33
UNSPSC Code:
12352200
Assay:
≥98% (HPLC)
Form:
solid
Quality level:
100
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light
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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

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).

Packaging

Packaged under inert gas

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

Disclaimer

Toxicity: Regulatory Review (Z)

Storage Class

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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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

Global Trade Item Number

SKUGTIN
373226-5MG04055977190984