HJB97

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) .

Product Specifications

CAS Number

[2093391-24-1]

UNSPSC

12352005

Target

Epigenetic Reader Domain; Ligands for Target Protein for PROTAC

Type

Reference compound

Related Pathways

Epigenetics; PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/HJB97.html

Purity

98.05

Solubility

DMSO : 30 mg/mL (ultrasonic)

Smiles

O=C(C1=NC(NC2=CC(C3CC3)=NN2CC)=C4C(NC5=C4C=C(OC)C(C6=C(C)ON=C6C)=C5)=N1)NC

Molecular Formula

C26H28N8O3

Molecular Weight

500.55

References & Citations

[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.|[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.