brd4bd2

MZP-54 is a selective degrader of BRD3/4 based on PROTAC technology(Kd of 4 nM for Brd4BD2)

MZP-55 is a selective BRD3/4 degrader based on PROTAC technology(Brd4BD2 with Kd of 8 nM)

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.

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.

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.

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.

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.

BRD4 Inhibitor-27 is a potent BRD4 inhibitor that inhibits BRD4 BD1 and BRD4 BD2 with IC50s of 9.6 and 11.3 μM, respectively.BRD4 Inhibitor-27 has anticancer activity and can be used for breast cancer research.

GNE-987 is a highly active chimeric BET degrader that binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low-nanomolar affinity and induces exceptionally potent BRD4 degradation in cells, achieving picomolar DC50 values in EOL-1 acute myeloid leukemia cells, thereby serving as a powerful chemical biology tool for dissecting BET-dependent transcriptional regulation.

MS402 is a novel BD1-selective BET BrD inhibitor.

(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.

CD161 is a potent, selective, and orally bioavailable BET bromodomain inhibitor (IC50s: 28.2 nM and 7.2 nM for BRD4 BD1 and BRD4 BD2) with good anticancer activity.

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).

INCB054329, a structurally distinct bromodomain and extraterminal domain (BET) inhibitor, inhibits BRD2-BD1, BRD2-BD2, BRD3-BD1, BRD3-BD2, BRD4-BD1, BRD4-BD2, BRDT-BD1 and BRDT-BD2 with IC50 values of 44 nM, 5 nM, 9 nM, 1 nM, 28 nM, 3 nM, 119 nM and 63 nM respectively.

GSK046 (iBET-BD2) is a potent, selective, and orally active BD2 bromodomain inhibitor of the BET proteins, with IC50 values of 264 nM [BRD2 BD2], 98 nM [BRD3 BD2], 49 nM [BRD4 BD2], and 214 nM [BRDT BD2], respectively. It exhibits immunomodulatory activity.

ABBV-744 is a BDII-selective BET bromodomain inhibitor that inhibits BRD2/3/4. It is used in the research on inflammatory diseases, cancer, and AIDS.

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.

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.

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

SJ46421, a PROTAC protein degrader derived from (+)-JQ-1, targets KLHDC2. It efficiently forms a stable ternary complex with KLHDC2, exhibiting an IC50 of 7.8 nM. Furthermore, SJ46421 promotes the polyubiquitination of the BD2 domain of BRD2, BRD3, or BRD4.

BRD4 Inhibitor-38 (Compound 25) is an orally active BRD4 inhibitor, exhibiting IC50 values of 3.64 μM for BRD4 BD1 and 0.12 μM for BRD4 BD2. It also demonstrates anti-inflammatory properties, with an IC50 value of 1.98 μM for nitric oxide (NO) production.

NB512 (compound 39a) is a dual inhibitor targeting both BET and HDAC, exhibiting high affinity for the BRD4 bromodomain and HDAC1/2, with EC50 values ranging from 100 to 400 nM. It demonstrates antiproliferative activity in cancer cell lines PaTu8988T and NMC.