brd4 (2)

(+)-JQ-1 (JQ1) is a specific, reversible BET bromine domain inhibitor that targets BRD4 (1 2) with IC50 values of 77 33 nM. (+)-JQ-1 induces cell autophagy and inhibits cell proliferation.

PROTAC BRD4 Degrader-2 is an efficacious degrader of PROTAC BRD4(BRD4 BD1,IC50 of 14.2 nM).

PROTAC BRD4 ligand-2 is a ligand for the target BRD4 protein used in the development of PROTAC CFT-2718.

PROTAC BRD4 Ligand-2 Hydrochloride serves as a ligand targeting the BRD4 protein, specifically designed for use with PROTAC CFT-2718.

PROTAC BRD3 BRD4-L degrader-2, a PROTAC molecule, selectively degrades cellular BRD3 and BRD4-L with K i values of 16.91 and 2.8 nM, respectively, and exhibits robust antitumor activity in mouse xenograft models, serving as a research tool for cancer [1].

ARV-771 is an effective BET degrader based on PROTAC technology. The Kd for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1) and BRD4(2) are 34 and 4.7 respectively. , 8.3, 7.6, 9.6 and 7.6 nM.

JQ-1 (carboxylic acid) is a cell-permeable BRD4 inhibitor with IC50s of 77 nM for BRD4(1) and 33 nM for BRD4(2)

I-BET762 carboxylic acid is an inhibitor of BRD4(pIC50 of 5.1).

Lenalidomide-PEG1-azide is an E3 ligase ligand-linker conjugate that incorporates the cereblon ligand based on Lenalidomide and a linker. It is designed for use in the development of PROTAC BRD4 Degrader-2[1].

PROTAC BRD2 BRD4 degrader-1 (compound 15) is a potent, selective degrader of BET proteins BRD4 and BRD2, achieving rapid, reversible, and unexpectedly selective elimination compared to BRD3. It effectively suppresses solid tumors with minimal cytotoxic effects and comprises a BET inhibitor, a connecting linker, and thalidomide as the ligand for cereblon (CRBN) cullin 4A[1].

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].

MZ 1 is a BRD4 protein degrader based on PROTAC technology.

PROTAC BRD4 Degrader-17 (compound 13i), a potent inhibitor, exhibits IC50 values of 29.54 nM (BRD4 (BD1)) and 3.82 nM (BRD4 (BD2)), effectively reducing Cyclin B1 expression linked with G2 M phase progression and significantly inducing apoptosis in MV-4-11 cells [1].

Tz-Thalidomide is a tetrazine-modified Thalidomide (E3 ligase ligand) with some affinity for BRD4.

MS83 is a proof-of-concept proteolysis-targeting chimera (PROTAC) that links a KEAP1 ligand with a binder for BRD4 3 2.

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.