protaclinkerconjugatesforpac

PAC is a chemical conjugate consisting of an ADCs linker and PROTACs linked to an antibody. When PAC is conjugated to an antibody, it exhibits enhanced degradation of estrogen receptor-alpha (ERα) in comparison to PROTAC alone.

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.

MC-(β-Ala)-PABC-(β-D-GlcUA)-amide-PEG1-CH2-CC-885 (Comp Ie) serves as a neodegrader conjugate instrumental in the synthesis of antibody neoDegrader conjugate (AnDC) [1].

MC-GGFG-DX8951 (MC-GGFG-Exatecan) is an antibody-coupled drug (ADC) drug-linker conjugate (DLC) consisting of DX8951, a potent DNA topoisomerase I inhibitor, the linker MC, and the cleavable peptide chain GGFG, and has antitumor potential.

PROTACBTK Degrader-8 (compound 3) is an efficient PROTAC BTK degrader with a linker that can couple with ADC antibodies to form PAC.

E3LigaseLigand-linker Conjugate 214 is an E3 ligase ligand-linker complex consisting of a Von Hippel-Lindau (VHL) ligand and a linker. This conjugate can bind with a target protein ligand to form a PROTAC molecule, specifically the PROTACLSD1 Degrader 1.

PROTAC BRD4 Degrader-13 (compound 9d) is a bioactive compound functioning as a proteolysis targeting chimera (PROTAC) by linking ligands for von Hippel-Lindau and BRD4 proteins. In PC3 prostate cancer cells, it effectively degrades the BRD4 protein through conjugation with STEAP1 and CLL1 antibodies, exhibiting a DC50 of 0.025 nM and 6.0 nM, respectively.

PROTAC BRD4 Degrader-11 (compound 9a), a PROTAC linked through ligands to von Hippel-Lindau and BRD4, effectively targets and degrades the BRD4 protein in PC3 prostate cancer cells when conjugated with STEAP1 and CLL1 antibodies, exhibiting potent activity with DC50 values of 0.23 nM and 0.38 nM for the respective conjugations [1].

PROTAC BRD4 Degrader-12 (compound 9c) is a PROTAC that links von Hippel-Lindau and BRD4 ligands. When conjugated with STEAP1 and CLL1 antibodies, this compound effectively degrades BRD4 protein in PC3 prostate cancer cells, demonstrating potent activity with DC50 values of 0.39 nM and 0.24 nM, respectively [1].

cBu-Cit-PROTAC BRD4 Degrader-5, a cBu-Cit conjugated PROTAC degrader, effectively degrades BRD4 in both HER2 positive and negative breast cancer cell lines.