PEG

Pomalidomide-C2-OH is a PROTAC linker featuring pomalidomide with an N-ethyl alcohol. Pomalidomide is a ligand for E3 ligase, which ubiquitinylates proteins and commits them to proteolytic destruction. Meanwhile, the hydroxyl is a versatile handle for forming more complex structures through a number of reactions.

2-(2,6-dioxopiperidin-3-yl)-4,5,6,7-tetrafluoro-2,3-dihydro-1H-isoindole-1,3-dione is a fluorinated thalidomide analogue. This molecule is an activator of E3 ligase, which ubiquitinylates proteins for later proteolysis. The structure may be further derivatized via substitution at its fluorines.

ARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity.

Thalidomide-O-PEG1-OH is a PROTAC linker featuring thalidomide with an O-ethyl alcohol. Thalidomide is a ligand for E3 ligase, which ubiquitinylates proteins, thus committing their fate to proteolytic destruction. Meanwhile, the hydroxyl is a versatile handle for forming more complex structures through a number of reactions.

2-(2,6-Dioxopiperidin-3-yl)-4,5-difluoroisoindoline-1,3-dione is a fluorinated thalidomide analogue. Thalidomide promotes the ubiquitinylation of proteins. The structure may be further derivatized via substitution at its fluorines.

5-amino-2-(1-methyl-2,6-dioxopiperidin-3-yl)-2,3-dihydro-1H-isoindole-1,3-dione is an aminated thalidomide analogue. E3 Ligase activators such as this may be used in the design of PROTAC molecules via derivatization at its amine.

4-(4-azidobutylamino)-2-(2,6-dioxo-3-piperidyl)isoindoline-1,3-dione is a PROTAC linker featuring pomalidomide with an N-butyl azide. Pomalidomide recruits E3 ligase for the ubiquitinylation of target proteins. Meanwhile, azide groups might be used in click chemistry to react with terminal alkynes or strained cyclooctynes.

2-(2,6-dioxopiperidin-3-yl)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)isoindoline-1,3-dione is a thalidomide analogue featuring a boronic pinacol ester, otherwise known as a Bpin group, and they are most frequently used in Suzuki reactions. This molecule is an activator for E3 ligase, which ubiquitinylates proteins, thus committing their fate to proteolytic destruction.

2-(2-Aminoethoxy)-N-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)acetamide, HCl salt is a crosslinker-E3 ligase ligand conjugate, consisting of an E3 ligase ligand pomalidomide and a PEGylated crosslinker with terminal amine for reactivity with a carboxyl group on the target ligand.