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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. 了解 Tocris 化合物库的更多信息。
分子量 | 414.33 |
公式 | C18H23N5O2.2HCl |
储存 | Desiccate at RT |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 37.79 | 100 | |
DMSO | 3.78 | 10 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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.
关键词: 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!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
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