brd2-bd1

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.

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).

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.

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.

KB-0118 (BBC0115) is an inhibitor targeting the BET bromodomain. It selectively binds to BRD2 and BRD4, with dissociation constants (Kd) of 36.7 μM for BRD2 BD1 and 47.4 μM for BRD4 BD1, while not binding to BRD3. KB-0118 suppresses the secretion of pro-inflammatory cytokines such as TNF, IL-1β, and IL-23a, and selectively inhibits Th17 cell differentiation. The compound regulates Th17-driven inflammation through the epigenetic suppression of BRD4, as evidenced by the downregulation of STAT3 and BRD4 target genes. Additionally, KB-0118 exhibits immunomodulatory effects in inflammatory bowel disease (IBD) models.

CZL-077 is a potent, highly selective, and orally active p300/CBP bromodomain (BRD) inhibitor, with p300 IC50 at 0.034 μM and CBP IC50 at 0.052 μM, demonstrating strong selectivity for the BRD of BET proteins (BRD2/3/4). This compound effectively inhibits the growth of OPM-2 and 22RV1 cells, with IC50 values of 0.024 μM and 5.6 μM, respectively. In xenograft mouse models of OPM-2 and 22RV1, CZL-077 exhibits anti-tumor activity. CZL-077 is applicable for research in multiple myeloma and prostate cancer.

BRD2 BD1 ligand-1 is an effective BRD2 BD1 binder (Ligands for Target Protein forPROTACs) and can be utilized in the synthesis of PROTAC BRD2 BD1 Degrader-1.

PROTACBRD2 BD1 Degrader-1 (compound 21-1) is a potent and selective PROTAC degrader targeting BRD2 BD1. It facilitates the interaction between BRD2 BD1 and von Hippel–Lindau-elongin C-elongin B (VCB).

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

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

BRD4 Inhibitor-25, a chemical compound targeting the BD1 and BD2 domains of BRD4 with half-maximal inhibitory concentrations (IC50s) of 0.82 μM and 1.94 μM respectively, demonstrates efficacy in inducing apoptotic and autophagic cell death in ovarian cancer cells. This compound is utilized in researching cancers, cardiovascular, neuromuscular, and inflammatory disorders.

SJ1461 is a potent, orally active inhibitor of the BET family, selectively targeting and inhibiting BRD2 (BD1), BRD2 (BD2), BRD4 (BD1), and BRD4 (BD2) with respective IC50 values of 1.6 nM, 0.1 nM, 6.5 nM, and 0.2 nM [1].

BET BD2-IN-1 (compound 45) is a potent and selective BET BD2 inhibitor with an IC50 value of 1.6 nM. It suppresses Th17 cell differentiation by reducing the activation of STAT3 and NF-κB, making it relevant for psoriasis and inflammatory bowel disease (IBD) research [1].

GSK778 hydrochloride hydrochloride is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 hydrochloride hydrochloride phenocopies the effects of pan-BET inhibitors in cancer models[1].

PLX51107 is a potent and selective BET inhibitor with Kds of 1.6, 2.1, 1.7, and 5 nM for BRD2-BD1, BRD3-BD1, BRD4-BD1, and BRDT-BD1, respectively.

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.

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).

PARP1/BRD4-IN-3 (compound HF4) is an effective inhibitor of BRD4 and PARP1, with IC50 values of 1210 nM and 2019 nM respectively. The compound exhibits antiproliferative activity, induces apoptosis (apoptosis) and cell cycle arrest at the G0/G1 phase. Additionally, PARP1/BRD4-IN-3 causes DNA damage and reduces the expression of the Rad51 protein, demonstrating anti-tumor activity.

BET-IN-27 (compound 6C) is an orally active BET inhibitor with IC50 values of 3.3 nM (BRD4-BD2), 3.4 nM (BRD4-BD1), 4.1 nM (BRD2-BD1), 20.4 nM (BRD3-BD1), and 42.0 nM (BRDT-BD1). It also exhibits antiproliferative activity.

XY221 (Compound 16o) selectively inhibits BRD4 BD2 with an IC50 of 5.8 nM. It demonstrates high selectivity for pan-BD2 and BRD4 BD2 domains, being 667 times more selective than for BRD4 BD1, and 9-32 times more selective than for BRD2/3/T BD2. XY221 can induce apoptosis in MV4-11 cells and exhibits anti-cancer activity.

BRD4 Inhibitor-40 (Compound 23) functions as an inhibitor of BRD, effectively targeting BRD4-BD1, BRD4-BD2, BRD2-BD1, and BRD2-BD2, with IC50 values of 16.1, 142.18, 29.35, and 302.35 nM, respectively. It modulates the expression of c-Myc and p21, induces cell cycle arrest in the G1 phase, and inhibits Pkd1-deficient (PN) renal cystic epithelial cells. Additionally, it prevents renal cyst formation in both Madin-Darby canine kidney and embryonic kidney cyst models, and demonstrates renal cyst inhibition activity in mouse models.

BRD4-IN-11 is an orally active and selective inhibitor of BRD4 with an IC50 of 26.35 nM for BD1 and 72.81 nM for BD2. Its potency against BRD4 is approximately 3 to 18 times greater than against BRr2, BRD3, and BRDT. BRD4-IN-11 increases H2S release and inhibits the upregulation of fibrosis markers (α-SMA and fibronectin), c-Myc, and CDC25B. It also reduces apoptosis in LO2 hepatic cells. In liver and lung fibrosis models, BRD4-IN-11 significantly improves liver and lung function, making it suitable for research on liver and lung fibrosis.