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Submit ReviewHLI 373 is an 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.
HLI 373 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
M. Wt | 414.33 |
Formula | C18H23N5O2.2HCl |
Storage | Desiccate at RT |
Purity | ≥99% (HPLC) |
CAS Number | 1782531-99-0 |
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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
water | 37.79 | 100 | |
DMSO | 3.78 | 10 |
The following data is based on the product molecular weight 414.33. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
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 |
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for HLI 373, please let us know.
Keywords: HLI 373, HLI 373 supplier, Hdm2, inhibitors, inhibits, inhibitor, p53, transcription, activators, HLI373, Ubiquitin, E3, Ligases, 3503, Tocris Bioscience
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:
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.
Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia