Biotin-Ahx-Ub-PA
a potent and specific inhibitor of deubiquitylating enzymes (DUBs), labeled on the N-terminus with biotin and a C-terminal propargylamide (PA) electrophile.
Additional information
| Weight | 0.05 kg |
|---|---|
| aliquot size | |
| Custom Aliquot size | |
| bulk size | |
| Applications | Crystallization, Pull down, Purification, Western Blot, MS, NMR, Phenotypic protein profiling |
| target | |
| source | |
| shipping | |
| purity | |
| molecular weight | |
| storage | upon arrival, powder at −20°C; buffered solution at −80°C. Please avoid multiple freeze/thaw cycles. |
| sample preparation | For detailed sample preparation see product sheet. |
| regulatory statement |
€220.00
- Description
- Additional information
- references
Description
Biotin-Ahx-Ub-PA (UbiQ-076) is a potent and specific inhibitor of deubiquitylating enzymes (DUBs), which is labeled on the N-terminus with biotin and contains a C-terminal propargylamide (PA) electrophile.
An aminohexanoic acid linker is used to create extra space between the biotin and Ub protein for efficient access of biotin binding entities.
This activity probe can be used for activity profiling experiments and determining DUB inhibitor specificity.
The C-terminal propargylamide (PA) electrophile has two characteristics:
1. it forms a covalent linkage with (the active site Cys residue of) a DUB that can be cleaved by acid treatment (5% aq. TFA), allowing for proteomic analyses.
2. it targets all three major DUB families: UCH, USP and OTU.
Additional information
| Weight | 0.05 kg |
|---|---|
| aliquot size | |
| Custom Aliquot size | |
| bulk size | |
| Applications | Crystallization, Pull down, Purification, Western Blot, MS, NMR, Phenotypic protein profiling |
| target | |
| source | |
| shipping | |
| purity | |
| molecular weight | |
| storage | upon arrival, powder at −20°C; buffered solution at −80°C. Please avoid multiple freeze/thaw cycles. |
| sample preparation | For detailed sample preparation see product sheet. |
| regulatory statement |
de Jong, A., et al. Ubiquitin-based probes prepared by total synthesis to profile the activity of deubiquitinating enzymes. ChemBiochem 13, 2251-2258 (2012).
http://www.ncbi.nlm.nih.gov/pubmed/23011887
Altun, M., et al. Activity-based chemical proteomics accelerates inhibitor development for deubiquitylating enzymes. Chem. Biol. 18, 1401-1412 (2011).
http://www.ncbi.nlm.nih.gov/pubmed/22118674
Ekkebus, R., et al. On terminal alkynes that can react with active-site cysteine nucleophiles in proteases. J. Am. Chem. Soc. 135, 2867-2870 (2013).
http://www.ncbi.nlm.nih.gov/pubmed/23387960
Sommer, S., et al. Covalent inhibition of SUMO and ubiquitin-specific cysteine proteases by an in situ thiol-alkyne addition. Bioorg. Med. Chem. 21, 2511-2517 (2013).
http://www.ncbi.nlm.nih.gov/pubmed/23535560