brd2

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].

NHWD-870 is an effective and selective inhibitor of BET family bromodomain only binding to BRD2, BRD3, BRD4 (IC50 = 2.7 nM), and BRDT. NHWD-870 exhibits potent anti-tumor efficacies and suppresses cancer cell-macrophage interaction through the increase of tumor apoptosis and inhibition of tumor proliferation.

CDD-1102 HCl is a novel BRDT-BD4 / BRD2-BD1302 selective inhibitor that shows non-hormonal contraceptive potential in ex vivo experiments.

GS-626510 is an orally bioavailable inhibitor of BET family bromodomains (Kd: 0.59-3.2 nM for BRD2/3/4; IC50: 83 nM and 78 nM for BD1 and BD2).

I-BET151 (GSK1210151A) (GSK1210151A) is a specific BET inhibitor for BRD2/3/4 (IC50: 0.5/0.25/0.79 μM, in cell-free assays).

GSK1324726A (I-BET726) is a greatly specific inhibitor of BET family proteins for BRD2(IC50=41 nM), BRD3(IC50=31 nM), and BRD4 (IC50=22 nM).

PFI-1 (PF-6405761), a specific BET (bromodomain-containing protein) inhibitor for BRD4, is with the IC50 of 0.22 μM in a cell-free assay.

Bromosporine is a broad spectrum inhibitor for bromodomains for BRD2/4/9 and CECR2 (IC50: 0.41/0.29/0.122/0.017 μM), 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.

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.

BET-IN-6, a ligand with potent and high affinity for inhibiting BRD2/BRD4, plays a crucial role in the synthesis of PROTAC BRD2/BRD4 degrader-1 [1], targeting the protein BRD2/4.

MS402 is a novel BD1-selective BET BrD inhibitor.

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.

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.

BRD20322 is a novel potent inhibitor of spCas9 that disrupts spCas9-DNA binding and exerts dose and temporal control of spCas9 in human cell lines. It reduces off-target DNA editing events, enhancing the precision and safety of CRISPR-Cas9 gene editing.

(iso)-BRD20322 is an isomer of BRD20322, a novel potent inhibitor of spCas9 that disrupts the binding of spCas9 to DNA and reduces non-specific DNA editing events, thereby improving the safety and accuracy of the CRISPR-Cas9 gene editing system.

BRD2577 is an HDAC inhibitor, by suppressing multiple HDAC enzymes and modulating acetylation levels in cells.

BRD2492 is a selective and potent dual inhibitor of HDAC1 and HDAC2 with potential anticancer, antitumour and antiproliferative activities, inhibiting HDAC1/2, HDAC3 and HDAC6.BRD2492 inhibits the growth of breast cancer cell lines and induces apoptosis.

BRD2879 is a potent and cell-active inhibitor of IDH1-R132H (IC50 = 50 nM).

BRD2889, an analog of the alkaloid piperlongumine, serves as a potent modulator of the GSTP1-ISCU axis in pulmonary hypertension (PH) [1].

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

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.