Protein degrader 1 hydrochloride

Protein degrader 1 hydrochloride is used in the synthesis of HaloPROTACs.

Signaling Pathways >> PROTAC >> PROTAC

Research Areas >> Others

Small molecule-induced protein degradation is an attractive strategy for the development of chemical probes.Protein degraders have the power to abrogate all of the functions of a drug target at once, including scaffolding functions which are difficult to target with small molecule inhibitors. A novel class of PROTACs that incorporate small molecule VHL ligands to successfully degrade HaloTag7 fusion proteins is developed. HaloPROTACs will inspire the development of future PROTACs with more drug-like properties. In HEK 293 cellsstably expressing GFP-HaloTag7,24 hour treatment with HaloPROTAC1 leads to less than 20% degradation, the longer HaloPROTAC2 leads to nearly 70% degradation of GFP-Halotag7 at 2.5 μM.HaloPROTACs containing protein degrader 1 leads to nearly 70% degradation of GFP-HaloTag7, when sufficiently long linkers are used[1].

[1]. Buckley DL, et al. HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins.ACS Chem Biol. 2015 Aug 21;10(8):1831-7.

ARV-771 | ARV-825 | dBET1 | dBET6 | Mz1 | BETd-260 | VH032-PEG5-C6-Cl (HaloPROTAC 2) | PROTAC 6 | Target Protein-binding moiety 4 | dTRIM24 | MZP-54 | PROTAC BET degrader-2 | PROTAC BRD9-binding moiety 1