PROTACs (PROteolysis TArgeting Chimeras) are heterobifunctional small molecules containing binding moieties for an E3 ubiquitin ligase and a target protein joined by a linker. PROTACs induce targeted protein degradation via the ubiquitin proteasome system. The binding of both moieties results in the formation of a ternary complex between target protein and E3 ligase, leading to polyubiquitination of the target protein, its recognition by the proteasome and subsequent degradation. A key feature of PROTACs is their catalytic mode of action. They dissociate following ubiquitination and rebind to new target proteins, which allows their use at sub-stoichiometric concentrations.
Catalog No. | Name |
---|---|
6P13119 | dBET1 |
6P15119 | MS4077 |
6P15219 | MS4078 |
6P13170 | (+)-JQ1 |
6P15170 | Ceritinib |