Biological Activity
Inhibitor of ubiquitin C-terminal hydrolase-L1 (UCH-L1) activity (Ki = 0.4 μM). Causes cell death through the apoptosis pathway; increases levels of highly ubiquitinated proteins and decreases ubiquitin proteasome activity. Activity leads to dramatic alterations in synaptic protein distribution and spine morphology in vivo.
Technical Data
| M. Wt | 397.64 |
| Formula | C17H11Cl3N2O3 |
| Storage | Desiccate at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 668467-91-2 |
| PubChem ID | 24906255 |
| InChI Key | OPQRFPHLZZPCCH-UHFFFAOYSA-N |
| Smiles | ClC1=CC=C(N(CC3=CC(Cl)=CC=C3Cl)C(C2=NOC(C)=O)=O)C2=C1 |
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 | 19.88 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 397.64. 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.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.51 mL | 12.57 mL | 25.15 mL |
| 5 mM | 0.5 mL | 2.51 mL | 5.03 mL |
| 10 mM | 0.25 mL | 1.26 mL | 2.51 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
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References
References are publications that support the products' biological activity.
Liu et al (2003) Discovery of inhibitors that elucidate the role of UCH-L1 activity in the H1299 lung cancer cell line. Chem.Biol. 10 837 PMID: 14522054
Tan et al (2008) Endoplasmic reticulum stress contributes to the cell death induced by UCH-L1 inhibitor. Mol.Cell.Biochem. 318 109 PMID: 18622688
Cartier et al (2009) Regulation of synaptic structure by ubiquitin C-terminal hydrolase L1. J.Neurosci. 29 7857 PMID: 19535597
Keywords: LDN 57444, supplier, LDN57444, UCH, L1, inhibitors, inhibits, ubiquitin, C-terminal, hydrolases, UCH-L1, Deubiquitinating, Enzymes, Deubiquitinating, Enzymes, Tocris Bioscience
