PROTAC BRD4 Degrader-5-CO-PEG3-N3

PROTAC BRD4 Degrader-5-CO-PEG3-N3 is a PROTAC-linker conjugate designed for targeted degradation of bromodomain-containing protein 4 (BRD4). It consists of a BRD4-targeting degrader connected to a PEG3-based linker terminating in an azide (N₃) functional group. The azide group provides a versatile handle for click-chemistry conjugation, including copper-catalyzed azide–alkyne cycloaddition (CuAAC) with alkyne-containing molecules and strain-promoted azide–alkyne cycloaddition (SPAAC) with DBCO- or BCN-containing molecules. This design enables incorporation of the BRD4 degrader into antibody-PROTAC conjugates and other targeted delivery systems.

The chemical name of PROTAC BRD4 Degrader-5-CO-PEG3-N3 is (3R,5S)-1-((S)-2-(tert-butyl)-17-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-4,16-dioxo-6,9,12-trioxa-3,15-diazaheptadecanoyl)-5-(((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)carbamoyl)pyrrolidin-3-yl 2-(2-(2-(2-azidoethoxy)ethoxy)ethoxy)acetate. The compound has a CAS No. of 2704602-92-4, a molecular formula of C₅₈H₇₅ClN₁₂O₁₂S₂, and a molecular weight of 1231.87 g/mol.

PROTAC BRD4 Degrader-5-CO-PEG3-N3 is intended for research applications involving BRD4 degradation, targeted protein degradation, PROTAC technology, click chemistry, bioconjugation, and antibody-PROTAC conjugate (PAC) development. It has been investigated as a conjugatable BRD4-degrading payload for HER2-targeted systems and research related to HER2-positive breast cancer. For research use only.