brd4-bd1

BRD4-BD1-IN-2 is a selective and potent BRD4-BD1 inhibitor with an IC50 value of 2.51 µM, exhibiting 20-fold greater inhibitory activity against BRD4-BD1 compared to BRD4-BD2. [BRD4-BD1-IN-2] is applicable for research in cardiovascular and cancer-related diseases.

CF53 is a highly potent, selective, and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM, and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, being very selective over non-BET bromodomain-containing proteins. CF53 exhibits potent anti-tumor activity both in vitro and in vivo.

MS417 (GTPL7512) is an inhibitor of BET-specific BRD4(BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively), with weak selectivity at CBP BRD with IC50 of 32.7 μM.

BRD4 Inhibitor-20 is a potent bromodomain protein 4 (BRD4) inhibitor with oral activity, demonstrating antiproliferative effects in cancer cell lines and used in studies of various cancers, including colon cancer.

MS402 is a novel BD1-selective BET BrD inhibitor.

BRD4 Inhibitor-10 is an inhibitor of BRD4-BD1 (IC50: 8 nM).

HJB97 is used for the design of potential PROTAC BET degrader. It also has antitumor activity. HJB97 is a high-affinity inhibitor of BET (Kis: 0.9 nM (BRD2 BD1), 0.27 nM (BRD2 BD2), 0.18 nM (BRD3 BD1), 0.21 nM (BRD3 BD2), 0.5 nM (BRD4 BD1), 1.0 nM (BRD4 BD2), respectively).

GSK778 is a potent and selective inhibitor of BD1 bromodomain such as BRD2 BD1 (IC50s = 75 nM), BRD3 BD1 (IC50s = 41 nM), BRD4 BD1 (IC50s = 41 nM), and BRDT BD1 (IC50s = 143 nM). GSK778 inhibits proliferation, induces a cell cycle arrest and apoptosis.

BRD4-BD1 2-IN-1 is a highly effective inhibitor of BRD4, targeting the BRD4 BD-1 and BD-2 domains with IC50 values of <100 nM each (US20150148375A1, compound 5) [1].

BRD4-BD1-IN-1 (Compound 9a) is a BRD4-BD1 inhibitor with an IC50 of 38.20 μM.

BRD4-BD1 2-IN-2 is a potent inhibitor of BRD4-BD2, effective on both BRD4 BD2 (IC50 < 0.5 nM) and BRD4 BD1 (IC50 < 300 nM).

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.

iBRD4-BD1 is a selective inhibitor of the BRD4 bromodomain, exhibiting inhibition activity with an IC50 value of 12 nM. It is utilized in the research of inflammation and oncology.

iBRD4-BD1 diTFA is a selective BRD4 bromodomain inhibitor with an IC50 value of 12 nM. It can be used for research in inflammation and oncology [1].

BY27, a potent and selective BET BD2 inhibitor (Ki: 3.1 nM) with anticancer activity, inhibits BD1/BD2 of BRD2, BRD3, BRD4, and BRDT, and suppresses tumor growth.

ZEN-3411 is an orally available and potent BET inhibitor that inhibits BRD4(BD1), BRD4(BD2), and BRD4(BD1BD2) and suppresses the growth of tumor cells overproducing BET proteins.

(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).

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.

NI-42 is a structurally orthogonal chemical probe for the BRPFs and is biased. It effective inhibitor of the BRD of the BRPFs (IC50s of BRPF1/2/3=7.9/48/260 nM; Kds of BRPF1/2/3=40/210/940 nM). It also has excellent selectivity over nonclass IV BRD protei

LT052 is a selective and efficient BET BD1 inhibitor with anti-inflammatory activity. It mediates the BRD4 NF-κB NLRP3 inflammatory signaling pathway and can be used in gout arthritis research.

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

CPI-637 is a selective and cell-active benzodiazepinone CBP EP300 bromodomain inhibitor.

ZEN-3219 is a BET inhibitor, which has inhibitory effect on BRD4(BD1), BRD4(BD2) and BRD4(BD1BD2). ZEN-3219 has inhibitory effect on BRD4(BD1), The IC50 values of BRD4(BD2) and BRD4(BD1BD2) were 0.48, 0.16 and 0.47 μM, respectively. ZEN-3219 is a component of PROTAC molecule and can induce BRD4 degradation.

RVX-297 is a BD2 selective inhibitor of BET bromodomains. RVX-297 preferentially binds to the BD2 domains of the BET bromodomain and Extra Terminal (BET) family of protein.