HLI 373

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Cat.No. 3503 - HLI 373 | C18H23N5O2.2HCl | CAS No. 502137-98-6
Description: Hdm2 inhibitor; activates p53-dependent transcription
Chemical Name: 5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dione dihydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Inhibitor of Hdm2 ubiquitin ligase (E3). Blocks Hdm2-mediated ubiquitylation and proteasomal degradation of p53; activates p53-dependent transcription. Induces apoptosis in several tumor cell lines that express wild-type p53 such as LOX-IMVI, A549, HT1080 and U2OS.

Technical Data

M. Wt 414.33
Formula C18H23N5O2.2HCl
Storage Desiccate at RT
Purity ≥99% (HPLC)
CAS Number 502137-98-6
PubChem ID 72193867
InChI Key WUEMKAQTAIRDOA-UHFFFAOYSA-N
Smiles CN2C1=CC=CC=C1C(NCCCN(C)C)=C3C2=NC(N(C)C3=O)=O.Cl.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 3.78 10
water 37.79 100

Preparing Stock Solutions

The following data is based on the product molecular weight 414.33. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.41 mL 12.07 mL 24.14 mL
5 mM 0.48 mL 2.41 mL 4.83 mL
10 mM 0.24 mL 1.21 mL 2.41 mL
50 mM 0.05 mL 0.24 mL 0.48 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Kitagaki et al (2008) Targeting tumor cells expressing p53 with a water-soluble inhibitor of Hdm2. Mol.Cancer Ther. 7 2445 PMID: 18723490

Yang et al (2009) Targeting the ubiquitin-proteasome system for cancer therapy. Cancer Sci. 100 24 PMID: 19037995


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Literature in this Area

Programmed Cell Death

Programmed Cell Death Poster

There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.

Pathways for HLI 373

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