protac brd4 degrader-3

PROTAC BRD4 Degrader-3 is an efficacious degrader of PROTAC BRD4.

PROTACBRD4 degrader-30 is an ISOX-DUAL-based PROTAC degrader, targeting BRD4 with an IC50 value of 65 nM. It is used in research studies related to c-Myc oncoproteins and the pathophysiology of cancer cells.

PROTACBRD4 Degrader-32 (Compound 22) is a potent BRD4 PROTAC degrader with a DC50 of 0.20 nM. It employs a unique carbon-carbon linker to connect the BRD4 binding domain with the CRBN binding domain, forming a ternary complex that induces BRD4 ubiquitination and facilitates proteasomal degradation. PROTACBRD4 Degrader-32 holds promise for research into BRD4-related cancers, such as hematological malignancies.

PROTACBRD4 Degrader-33 is an enzyme-activated, click-responsive BRD4 PROTAC degrader designed with effective tumor microenvironment responsiveness. This compound exhibits exceptional penetration into tumor tissues and effectively inhibits PD-L1 protein expression. In the 4T1 tumor mouse model, PROTACBRD4 Degrader-33 demonstrates potent antitumor immunomodulatory activity.

PROTACBRD4 Degrader-31 is a BRD4 PROTAC degrader with DC50 values of 164 nM at 4 hours and 80 nM at 24 hours. It effectively degrades BRD4 within cells and exhibits long-lasting degradation kinetics.

PROTACBRD4 Degrader-35 (Compound 17) is a PROTAC degrader targeting BRD4. It is utilized in cancer research.

PROTACBRD4 Degrader-34 is a selective BRD4 PROTAC degrader (pDC50= 8.4) that induces VHL-mediated BD2 degradation and is applicable for cancer research.

PROTACBRD4 Degrader-36 (Compound TrimTAC-1) is a BRD4 PROTAC degrader. It has a DC50 of 0.649 nM and a Dmax of 71% in PANC-1 cells. Additionally, PROTACBRD4 Degrader-36 exhibits cytotoxicity towards PANC-1 cells with a GI50 of 0.103 μM. This compound is applicable for tumor research.

PROTACBRD4 Degrader-38 is a BRD4 PROTAC degrader with DC50 values of 86 nM and 106 nM for the short and long BRD4 isoforms, respectively. It significantly induces BRD4 degradation through covalent binding at the C232 site of the E3 ligase TRIM28.

PROTACBRD4 Degrader-37 is a PROTACBRD4 degrader with a DC50 of 36.4 nM and a Dmax of 73% in PANC-1 cells. It exhibits cytotoxicity against PANC-1 cells with a GI50 of 0.282 μM. PROTACBRD4 Degrader-37 is applicable for cancer research.

LO-3-61 is a JQ-1 analog featuring a truncated fumarylamide group, classified as a BRD4 degrader with PROTAC (protein degradation targeting chimera) properties. It promotes the degradation of both long and short BRD4 isoforms via a CUL4DCAF16-dependent pathway. In MDA-MB-231 cells, LO-3-61 exhibits selectivity in degrading BRD3 and BRD4.

Pomalidomide-PEG3-Cys is an E3 ubiquitin ligase ligand-linker conjugate, consisting of a CRBN ligand Pomalidomide and a three-unit PEG linker. It can be utilized in the synthesis of PROTAC BRD4 Degrader-33.

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-27 is a selective PROTAC targeting BRD4, distinguished from BRD2/BRD3. This compound is composed of the E3 ubiquitinase ligand Thalidomide-4-OH, the PROTAC Linker γ-Aminobutyric acid, and the PROTAC target protein ligand PROTAC BRD4 ligand-3. The active control for this target protein ligand is Mivebresib, while the conjugate of the E3 ubiquitin ligase ligand and Linker is identified as Pomalidomide 4'-alkylC3-acid.