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.

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.

PROTAC BRD4 Degrader-5-CO-PEG3-N3 is a PROTAC-linker conjugate for PAC. PROTAC BRD4 Degrader-5-CO-PEG3-N3 comprises the BRD4 degrader GNE-987 linked through a PEG-based spacer to enable modular bioconjugation. PROTAC BRD4 Degrader-5-CO-PEG3-N3 functions as a click-chemistry reagent containing an azide group capable of undergoing copper-catalyzed azide-alkyne cycloaddition (CuAAC) with alkyne-bearing molecules. PROTAC BRD4 Degrader-5-CO-PEG3-N3 can also react through strain-promoted alkyne-azide cycloaddition (SPAAC) with DBCO- or BCN-containing compounds, thereby supporting targeted PROTAC assembly and bioconjugation for chemical biology and drug-discovery applications.

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.

TKP-5 is a PROTAC protein degrader targeting BRD4. It binds to BRD2, BRD3, BRD4, and BRDT, with dissociation constants (Ka) of 150 nM, 100 nM, and 150 nM for the first three, respectively. TKP-5 inhibits thymic stromal lymphopoietin production and downregulates IL-33 mRNA expression. It is applicable for studies on tape-stripping-induced skin injury.

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.