an activity based probe for Ub E1, E2 and (HECT/RBR) E3 ligases, labeled with biotin on the N-terminus


code UbiQ-102 Category
product UbiQ-102 Category
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UbiQ-102 is an activity based probe for Ub E1, E2 and (HECT/RBR) E3 ligases [Mulder et al. 2016]. It is based on the Ub sequence in which the C-terminal Gly76 has been replaced by a dehydroalanine (Dha) residue. The N-terminus is labeled with biotin; an aminohexanoic acid (Ahx) linker is used to create extra space between the biotin and Ub protein for efficient access of biotin binding entities. It has been prepared by total chemical synthesis and is therefore well-defined in terms of biotinylation site.

UbiQ-102 is processed in a native manner by Ub E1, E2 and (HECT/RBR) E3 ligases and during this process, it forms an electrophilic intermediate that can react with the active site Cys residue of the E1, E2 and (HECT/RBR) E3 enzyme, thereby creating a covalent bond (see figure).

Mulder et al., A cascading activity-based probe sequentially targets E1–E2–E3 ubiquitin enzymes. Nature Chem Bio (2016)