bet proteins

Molibresib (GSK525762) is an inhibitor of BET proteins (IC50: about 35 nM).

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.

Hexamethylene bisacetamide inhibits BET Bromodomain Proteins.

The S-enantiomer of BET-BAY 002, referred to as BET-BAY 002 S enantiomer, is a potent inhibitor of BET (Bromodomain and Extra-Terminal motif proteins).

Molibresib besylate (GSK 525762C) is a selective and potent inhibitor of the bromodomain and extra-terminal (BET) family of proteins with potential anticancer activity for the study of refractory hematologic malignant diseases.Molibresib besylate generates reactive oxygen species (ROS), which potentiate ATM activation.

PROTAC BET degrader-2 is a highly potent degrader of Bromodomain and Extra-Terminal (BET) proteins, with an IC50 of 9.6 nM.

(R)-BAY1238097 represents the R-isomer of BAY1238097, which exhibits relatively lower activity compared to its counterpart. BAY1238097 is a highly potent and selective inhibitor targeting the binding of BET proteins to histones, demonstrating significant anti-proliferative effects in various acute myeloid leukemia (AML) and multiple myeloma (MM) models. The high activity is achieved through the down-regulation of c-Myc levels and the subsequent modulation of its downstream transcriptome.

(S,R,S)-AHPC-Me dihydrochloride, also known as VHL ligand 2 dihydrochloride, is a chemical compound used in the synthesis of ARV-771. ARV-771 is a BET PROTAC degrader that relies on von Hippel-Landau (VHL) E3 ligase and exhibits potent degradation of BET proteins in castration-resistant prostate cancer (CRPC) cells, with a DC50 of less than 1 nM. This compound acts as the VHL ligand, specifically the (S,R,S)-AHPC-based VHL ligand, facilitating the recruitment of von Hippel-Lindau (VHL) protein.

PROTAC BET Degrader-3 is a potent degrader of BET proteins based on the PROTAC (PROteolysis TArgeting Chimera) technology.

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].

Thalidomide-NH-C4-NH2 TFA (compound 29c) is a conjugate composed of an E3 ligase ligand-linker that integrates a Thalidomide-based cereblon ligand and a linker moiety. This compound is used as a component in PROTAC BRD2/BRD4 degrader-1, a highly potent and selective degrader targeting BET proteins BRD4 and BRD2[1].

BET-IN-28 (Compound 44) is a potent inhibitor of bromodomain and extra-terminal domain (BET) proteins, exhibiting an IC50 value of 4.47 nM for BRD4-BD1. It obstructs the interaction between BET proteins and the N-acetylated lysine residues on histone tails, leading to the downregulation of specific gene expression. BET-IN-28 is applicable in research related to hematologic malignancies and solid tumors.

BTR2004 is a selective PROTAC degrader targeting the BET family (BRD2/3/4) proteins. It facilitates the formation of a ternary complex with BRD proteins and KLHL20, leading to ubiquitination and proteasomal degradation via the UPS pathway. BTR2004 shows potential for research in PC3 prostate cancer and MDA-MB-231 breast cancer cell lines.

K2-B4-5e is a PROTAC compound designed to target the degradation of BRD4 and androgen receptor (AR) through a KLHDC2-based E3 ligase mechanism. It effectively induces rapid and potent degradation of BET family proteins and AR within cells.

IBG3 is a bifunctional BET molecular glue degrader containing two JQ1 moieties, designed to target and degrade proteins through an intramolecular bivalent mechanism. It acts as a degrader for BRD2 and BRD4, with DC50 values of 8.6 pM and 6.7 pM, respectively.

Progranulin modulator-2 (compound 18A) is a novel bromodomain and extra-terminal domain (BET) inhibitor. By targeting BET protein family members, Progranulin modulator-2 enhances PGRN expression. It is applicable for studying the role of BET proteins in neurodevelopment, neural plasticity, and neurodegeneration.

PROTACBET Degrader-12 (Compound 8b) is a PROTAC degrader targeting proteins with bromodomains and extraterminal (BET) domains, facilitating the degradation of BRD3 and BRD4 in a DCAF11-dependent manner. It inhibits the viability of KBM7 cells with a DC50 of 305.2 nM.

PROTACBET Degrader-13 (Compound 34) is a TRIM21-based PROTAC (TRIMTAC) degrader that targets BET proteins. It effectively degrades the PML-eGFP-BRD4 fusion protein, causing a near-complete loss of EGFP+ nuclear foci with an EC50 of 1.4 μM.

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.

PROTACBET Degrader-14 is a potent PROTAC compound designed to target BET (bromodomain and extraterminal domain) proteins. It effectively degrades all family members of BET, including BRD2, BRD3, and BRD4. The compound demonstrates significant efficacy in degrading BET proteins in the U2OS osteosarcoma cell line (BRD4 DC50 = 130 nM) and the KYSE180 esophageal squamous cell carcinoma cell line (DC50 = 40 nM). Its mechanism of degradation relies on the ubiquitin-proteasome system. Furthermore, PROTACBET Degrader-14 reduces the expression levels of BET-regulated gene products such as c-Myc, RUNX2, and KRT14, making it a valuable tool for osteosarcoma research.

EBET-1593 is a BETPROTAC degrader that facilitates the ubiquitination and degradation of BET proteins. It serves as the primary payload and can be utilized in the synthesis of ADCs, such as 84-EBET, which exhibits antitumor activity against pancreatic ductal adenocarcinoma.

GSK2820151 is an orally bioavailable inhibitor of the bromodomain and extra-terminal (BET) family of proteins with potential antineoplastic activity.

RX-37 is a potent BET inhibitor with Ki values of 3.2-24.7 nM for BRD2, BRD3 and BRD4. RX-37 demonstrates high selectivity over other non-BET bromodomain-containing proteins. RX-37 potently and selectively inhibits cell growth in human acute leukemia cell