brd4

PROTAC BRD4 Degrader-13 (compound 9d) is a bioactive compound functioning as a proteolysis targeting chimera (PROTAC) by linking ligands for von Hippel-Lindau and BRD4 proteins. In PC3 prostate cancer cells, it effectively degrades the BRD4 protein through conjugation with STEAP1 and CLL1 antibodies, exhibiting a DC50 of 0.025 nM and 6.0 nM, respectively.

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].

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

PROTAC BRD4 Degrader-9 (compound 8a) is a novel chemical compound comprising ligands for von Hippel-Lindau and BRD4, connected by a PROTAC moiety. This compound efficiently degrades the BRD4 protein in PC3 prostate cancer cells. When conjugated with STEAP1 and CLL1 antibodies, PROTAC BRD4 Degrader-9 exhibits potent activity, with respective DC50 values of 0.86 nM and 7.6 nM.

PROTAC BRD4 Degrader-15 is a chemical compound consisting of a PROteolysis TArgeting Chimera (PROTAC) linked to ligands specific to von Hippel-Lindau and BRD4. It exhibits an IC50 of 7.2 nM for BRD4 BD1 and 8.1 nM for BRD4 BD2 and demonstrates potent degradation activity against the BRD4 protein in PC3 prostate cancer cells.

PROTAC BRD4 Degrader-5 is a PROTAC-based compound that efficiently degrades BRD4 in both HER2-positive and HER2-negative breast cancer cell lines[1].

PROTAC BRD4 ligand-1, a component of Protac GNE-987, is a ligand for BRD4 and acts as an inhibitor of BET.

PROTAC BRD4 Degrader-16 is a potent degrader of BRD4, with IC50 values of 34.58 nM for BRD4 (BD1) and 40.23 nM for BRD4 (BD2). It significantly reduces Cyclin B1 expression, impedes G2 M phase progression, and induces apoptosis in MV-4-11 cells [1].

PROTAC BRD4 Degrader-22 (Compd 44h) is a PROTAC-based degrader targeting BRD4, with a pDC50 of 9.2 in MOLT4 cells over 24 hours [1].

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

PROTAC BRD4 Degrader-12 (compound 9c) is a PROTAC that links von Hippel-Lindau and BRD4 ligands. When conjugated with STEAP1 and CLL1 antibodies, this compound effectively degrades BRD4 protein in PC3 prostate cancer cells, demonstrating potent activity with DC50 values of 0.39 nM and 0.24 nM, respectively [1].

PROTAC BRD4 Degrader-14, a PROTAC (Proteolysis Targeting Chimera) linked by ligands to von Hippel-Lindau and BRD4, exhibits IC50 values of 1.8 nM and 1.7 nM for BRD4 BD1 and BD2, respectively. This compound effectively degrades the BRD4 protein in PC3 prostate cancer cells [1].

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].

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.

PROTAC BRD4 Degrader-1 is an efficacious degrader of BRD4(BRD4 BD1,IC50 of 41.8 nM).

PROTAC BRD4 Degrader-20 (compound 195) is a bifunctional degrader of BRD4 [1].

PROTAC BRD4 Degrader-11 (compound 9a), a PROTAC linked through ligands to von Hippel-Lindau and BRD4, effectively targets and degrades the BRD4 protein in PC3 prostate cancer cells when conjugated with STEAP1 and CLL1 antibodies, exhibiting potent activity with DC50 values of 0.23 nM and 0.38 nM for the respective conjugations [1].

BRD4 degrader AT1 is a highly selective Brd4 degrader based on PROTAC technology, with a Kd of 44 nM for Brd4BD2 in cells.

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-binding moiety 1 is a BRD4 ligand that binds to the cereblon ligand via a linker, facilitating the formation of a PROTAC complex which efficiently degrades BRD4[1].

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].

PROTAC BRD4 Degrader-21 (Comp 74), a potent BRD4 degrader, has shown significant inhibition of tumor growth in mouse xenograft models, indicating its potential for anticancer research [1].

PROTAC BRD4 Degrader-10, also known as compound 8b, is a dual ligand-based PROTAC that combines ligands for von Hippel-Lindau and BRD4. To degrade the BRD4 protein in PC3 prostate cancer cells, PROTAC BRD4 Degrader-10 can be conjugated with STEAP1 and CLL1 antibodies, with respective DC 50 values of 1.3 nM and 18 nM.

PROTAC BRD4 Degrader-19 (compound 176) is a proteolysis-targeting chimera (PROTAC) developed to specifically degrade the BRD4 protein, potentially useful in cancer research [1].

BRD4 Ligand-Linker Conjugate 1 is a compound consisting of a ligand and a linker, specifically designed to bind to the target protein BRD4. This conjugate serves as a valuable tool for synthesizing PROTACs, molecules utilized for targeted protein degradation.

PROTAC BRD4 Degrader-7, a potent bromodomain BRD4 inhibitor exemplified by compound 1a, demonstrates half-maximal inhibitory concentrations (IC50s) of 15.5 nM and 12.3 nM for BRD4-BD1 and BRD4-BD2, respectively [1].

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

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

Desmethyl-QCA276, the QCA276-based moiety, binds to cereblon ligand via a linker to form PROTAC to degrade BET. QCA276 is a BET inhibitor with an IC50 of 10 nM, and with a Ki of 2.3 nM[1].

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

(+)-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.

ARV-771 is a potent BET degrader based on PROTAC technology, with Kds of 34 nM for BRD2(1), 4.7 nM for BRD2(2), 8.3 nM for BRD3(1), 7.6 nM for BRD3(2), 9.6 nM for BRD4(1), and 7.6 nM for BRD4(2), respectively[1].

FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional compound that selectively degrades the BET bromodomain transcriptional co-activator BRD4 by linking BET bromodomains to the E3 ubiquitin ligase CRBN. It also functions as a degrader of FKBP12F36V when FKBP12F36V is expressed in-frame with a targeted protein.

QCA570 is an effective BET degrader based on PROTAC (IC50: 10 nM for BRD4 BD1 Protein).

BETd-260, a PROTAC linked by a Cereblon ligand and a BET ligand, has an inhibitory effect on BRD4 protein in leukemic cell lines.

dBRD4-BD1 is a selective BRD4 bromodomain inhibitor. dBRD4-BD1 can selectively degrade BRD4 (DC50 = 280 nM). Notably, dBRD4-BD1 upregulates BRD2/3, a result not observed with degraders using pan-BET ligands. Designing BRD4 selectivity up front enables analysis of BRD4 biology without wider BET-inhibition and simplifies designing BRD4-selective heterobifunctional molecules, such as degraders with new E3 recruiting ligands or for additional probes beyond degraders.

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

ZEN-3862 (Willardiine) is an inhibitor of BET(IC50s of 0.16 and 0.13 μM for BRD4(BD1) and BRD4(BD2) , respectively). ZEN-3862 can be used to form PROTACs to induce degradation of BRD4.

A1874 is a nutlin-based and BRD4-degrading PROTAC which induces BRD4 degradation in cells. Effective in inhibiting many cancer cell lines proliferation.

Azido-PEG1-CH2CO2H, a PROTAC linker characterized by an alkyl ether combination, can be utilized to synthesize PROTAC BRD4 Degrader-1[1].

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

AT6 is a PROTAC AT1 analog which is a highly selective bromodomain (Brd4) degrader.

(S)-GNE-987 binds to the BRD4 BD1(IC50=4 nM) and BD2 (3.9 nM) bromodomains and can be used to design PROTAC-Antibody Conjugate (PAC).

PROTAC BRD9 Degrader-1 is a leading PROTAC BRD9 chemical degrader with an IC50 of 13.5 nM.

(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.

PROTAC BET Degrader-10 (WO2017007612A1, example 37) is a highly efficient and selective small molecule compound designed to degrade BET protein BRD4. PROTAC BET Degrader-10 functions by utilizing specific ligands that connect Cereblon and BRD4, with a DC 50 value of 49 nM.

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