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Description: Proteasome inhibitor. Also prevents activation of NF-κB
Chemical Name: N-[(Phenylmethoxy)carbonyl]-L-isoleucyl-L-α-glutamyl-tert-butyl ester-N-[(1S)-1-formyl-3-methylbutyl]-L-alaninamide
Purity: ≥90% (HPLC)
Biological Activity for PSI
Proteasome inhibitor; inhibits chymotrypsin-like activity of the proteasome. Causes dopaminergic cell death in vitro. Prevents activation of NF-κB in response to TNF-α and okadaic acid (Cat. No. 1136) by inhibiting IκB-α degradation. Also inhibits NO production by LPS-activated macrophages.
Technical Data for PSI
| M. Wt | 618.77 |
| Formula | C32H50N4O8 |
| Storage | Store at -20°C |
| Purity | ≥90% (HPLC) |
| CAS Number | 158442-41-2 |
| PubChem ID | 9960660 |
| InChI Key | TYFTWYMXUWCOOB-YICLCXKGSA-N |
| Smiles | [H]C([C@H](CC(C)C)NC([C@H](C)NC([C@H](CCC(OC(C)(C)C)=O)NC([C@H]([C@@H](C)CC)NC(OCC1=CC=CC=C1)=O)=O)=O)=O)=O |
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.
Product Datasheets for PSI
References for PSI
References are publications that support the biological activity of the product.
Traenckner et al (1994) A proteasome inhibitor prevents activation of NF-κB and stabilizes a newly phosphorylated form of IκB-α that is still bound to NF-κB. EMBO J. 13 5433 PMID: 7957109
Bukhatwa et al (2009) An immunohistochemical and stereological analysis of PSI-induced nigral neuronal degeneration in the rat. J.Neurochem. 109 52 PMID: 19187437
Griscavage et al (1996) Inhibitors of the proteasome pathway interfere with induction of nitric oxide synthase in macrophages by blocking activation of transcription factor NF-κB. Proc.Natl.Acad.Sci.USA 93 3308
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Keywords: PSI, PSI supplier, proteasome, inhibitors, inhibits, Nuclear, Factor, Kappa, B, NF-κB, NF-kappaB, NF-kB, activation, Proteasome, NF-kB/IkB, 4045, Tocris Bioscience
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TPD and Induced Proximity Research Product GuideUpdated
This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:
- Active Degraders
- TAG Degradation Platform
- Degrader Building Blocks
- Assays for Protein Degradation
- Induced Proximity Tools
Targeted Protein Degradation Poster
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