protac brd4 degrader 5

PROTAC BRD4 Degrader-5 is a PROTAC that efficiently degrades BRD4 in HER2-positive and -negative breast cancer cell lines, and is formed by linking von Hippel-Lindau ligand to BRD4 ligand.

PROTAC BRD4 Degrader-5-CO-PEG3-N3 (Compound 2) is a PROTAC-linker conjugate utilized in PAC, comprising the BRD4 degrader GNE-987 connected with a 3-PEG linker. This compound serves as a click chemistry reagent, featuring an Azide group capable of undergoing copper-catalyzed azide-alkyne cycloaddition reactions (CuAAc) with molecules containing an Alkyne group. Additionally, it can participate in strain-promoted alkyne-azide cycloaddition reactions (SPAAC) with molecules that possess DBCO or BCN groups.

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.

dBRD9 HCl is a PROTAC composed of the BRD9 inhibitor BI 7273 conjugated to the cereblon E3 ligase ligand pomalidomide . dBRD9 HCl is a potent and selective degrader of BRD9 (IC50 = 56.6 nM in MOLM-13 cells). dBRD9 HCl does not degrade BRD4 or BRD7 at concentrations up to 5 μM. dBRD9 HCl displays antiproliferative effects in human AML cell lines.

PROTAC BRD4 Degrader-8 is a potent BRD4 inhibitor with IC50 values of 1.1 nM and 1.4 nM for BRD4 BD1 and BD2, respectively, effectively degrading the BRD4 protein in PC3 prostate cancer cells[1].

(S,R,S)-AHPC-Me-CO-CH2-PEG3-NH2 is a synthetic E3 ligase ligand-linker conjugate composed of a VHL ligand and a linker, utilized in PROTAC BRD4 Degrader-5 and PROTAC BRD4 Degrader-5-CO-PEG3-N3.