betin2

BET-IN-2 is a BET inhibitor with an IC50 of 52 nM for BRD4-BD1.

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.

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.

BET-IN-21 (compound 16) is a BET (Bromo and Extra-Terminal domain) inhibitor capable of penetrating the blood-brain barrier, with a Ki value of 230 nM. It suppresses microglial activation and demonstrates therapeutic effects in mice with experimental autoimmune encephalomyelitis.

BET-IN-26 (compound 13a) is a potent, selective, and orally active BD1 inhibitor, exhibiting IC50 values of 0.0055 µM for BD1 and 9.0 µM for BD2. It effectively reduces serum IL-6 and MCP-1 levels induced by LPS.

BET-IN-25 (compound 7) is an orally bioactive inhibitor targeting the bromodomains BD1 and BD2, with IC50 values of 0.18 μM and 9.2 μM, respectively.

BET-IN-20 (compound 10), a BRD4 BD1 inhibitor (IC 50 =1.9 nM), exhibits significant anticancer properties. It promotes apoptosis in acute myeloid leukemia (AML) cells and arrests the cell cycle in the G0/G1 phase. Additionally, BET-IN-20 inhibits both c-Myc and CDK6, and enhances PARP cleavage [1].

BET-IN-23 (Compound 23) is a BD2-selective BET inhibitor with an IC50 of 2.9 nM. It exhibits anticancer activity by significantly inhibiting the proliferation of acute myeloid leukemia (AML) cell lines, inducing G0/G1 arrest, and apoptosis in vitro [1].