GNE-987 is a highly active chimeric BET degrader. GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50: 4.7 and 4.4 nM, respectively). GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50: 0.03
NH2-PEG1-CH2CH2-Boc is a polyethylene glycol (PEG) and alkyl ether-based proteolysis targeting chimeric (PROTAC) linker, commonly employed in the synthesis of PROTACs[1].
β-Naphthoflavone-CH2-OH (β-NF-CH2-OH) serves as an AhR E3 ligase ligand, forming chimeric molecules when connected to a protein ligand through a linker, resulting in PROTACs or SNIPERs (e.g., β-naphthoflavone-JQ1). These chimeric molecules recruit the AhR E3 ligase complex by incorporating AhR ligands. By inducing ubiquitination-mediated degradation, PROTACs effectively target and degrade cancer-promoting proteins [1].
Azide-PEG-amine (MW 3500) is a polyethylene glycol (PEG) derived linker compound, specifically designed for the synthesis of proteolysis targeting chimeric molecules (PROTACs)[1].
PROTAC BRD4 degrader for PAC-1 (compound 5) is a chimeric BET degrader GNE-987 conjugated with a disulfide-containing linker[1]. This PROTAC-linker conjugate specifically targets and degrades BRD4, enabling selective proteolysis of PAC-1.
Tri(Amino-PEG3-amide)-amine is a polyethylene glycol (PEG)-derived linker employed for the synthesis of proteolysis-targeting chimeric molecules (PROTACs)[1].
GSK-2336805 is a HCV NS5A inhibitor. GSK2336805 retained activity on chimeric replicons containing NS5A patient sequences from genotype 1 and patient and consensus sequences for genotypes 4 and 5 and part of genotype 6.