DBET57

DBET57 is an effective and selective BRD4BD1 degrader based on PROTAC technology, with the ability to induce cell apoptosis and anti-tumor activity. dBET57 mediates the recruitment of the E3 ubiquitin ligase CRL4Cereblon, showing a DC50/5h value of 500 nM for BRD4BD1[1][2].

Product Specifications

CAS Number

[1883863-52-2]

UNSPSC

12352005

Hazard Statement

H302, H312, H315, H319, H332, H335

Target

Apoptosis; Epigenetic Reader Domain; PROTACs

Type

Reference compound

Related Pathways

Apoptosis; Epigenetics; PROTAC

Applications

Neuroscience-Neuromodulation

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/dbet57.html

Purity

99.94

Solubility

DMSO : 250 mg/mL (ultrasonic)

Smiles

O=C(NCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)C[C@H]4C5=NN=C(C)N5C6=C(C(C)=C(C)S6)C(C7=CC=C(Cl)C=C7)=N4

Molecular Formula

C34H31ClN8O5S

Molecular Weight

699.18

Precautions

H302, H312, H315, H319, H332, H335

References & Citations

[1]Nowak RP, et al. Plasticity in binding confers selectivity in ligand-induced protein degradation. Nat Chem Biol. 2018 Jul;14 (7) :706-714.|[2]Si-Qi Jia, et al. The BRD4 Inhibitor dBET57 Exerts Anticancer Effects by Targeting Superenhancer-Related Genes in Neuroblastoma. J Immunol Res. 2022 Nov 16:2022:7945884.