BETd-260

BETd-260 (ZBC 260) is a PROTAC connected by ligands for Cereblon and BET, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line[1]. BETd-260 potently suppresses cell viability and robustly induces apoptosis in hepatocellular carcinoma (HCC) cells[2].

Product Specifications

CAS Number

[2093388-62-4]

Product Name Alternative

ZBC 260

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Epigenetic Reader Domain; PROTACs

Type

Reference compound

Related Pathways

Apoptosis; Epigenetics; PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/BETd-260.html

Purity

99.68

Solubility

DMSO : 25 mg/mL (ultrasonic)

Smiles

CCN1N=C(C2CC2)C=C1NC3=NC(C(NCCCCCC4=CC=CC5=C4CN(C6C(NC(CC6)=O)=O)C5=O)=O)=NC7=C3C8=CC(OC)=C(C9=C(C)ON=C9C)C=C8N7

Molecular Formula

C43H46N10O6

Molecular Weight

798.89

Precautions

H302, H315, H319, H335

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]Zhang H, et al. Targeting BET Proteins With a PROTAC Molecule Elicits Potent Anticancer Activity in HCC Cells. Front Oncol. 2020;9:1471. Published 2020 Jan 14.