2093391-24-1

HJB97 is a high-affinity BET inhibitor with Ki values of 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), and 1.0 nM (BRD4 BD2)[1]. HJB97 can serve as a ligand for target protein (Ligands for Target Protein for PROTAC) for the development of PROTAC BET degraders with antitumor activity[1]. HJB97 can be used for the synthesis of BETd-260 (HY-101519).

BRD2 BD1: 0.9±0.2 nM (Ki); BRD2 BD2: 0.27±0.09 nM (Ki); BRD3 BD1: 0.18±0.01 nM (Ki); BRD3 BD2: 0.21±0.03 nM (Ki); BRD4 BD1: 0.5±0.2 nM (Ki); BRD4 BD2: 1.0±0.1 nM (Ki); BRD2 BD1: 3.1±0.7 nM (IC₅₀); BRD2 BD2: 3.9±0.5 nM (IC₅₀); BRD3 BD1: 6.6±0.2 nM (IC₅₀); BRD3 BD2: 1.9±0.4 nM (IC₅₀); BRD4 BD1: 7.0±0.6 nM (IC₅₀); BRD4 BD2: 7.0±0.1 nM (IC₅₀)

[1] Zhou B, et al. Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. J Med Chem. 2018 Jan 25;61(2):462-481. DOI:10.1021/acs.jmedchem.6b01816
[2] Wang C, et al. PROTACs for BRDs proteins in cancer therapy: a review. J Enzyme Inhib Med Chem. 2022 Dec;37(1):1694-1703. DOI:10.1080/14756366.2022.2081164