1883863-52-2
Chemical Structure
dBET57
- CAS No.: 1883863-52-2
- Formula:C34H31ClN8O5S
- Molecular Weight:699.18
IUPAC Name: 2-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-N-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethyl)acetamide
InChIKey: CZRLOIDJCMKJHE-UXMRNZNESA-N
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
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
dBET57 | 99.94% | 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. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
- [1]. 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. [Content Brief]
- [2]. Nowak RP, et al. Plasticity in binding confers selectivity in ligand-induced protein degradation. Nat Chem Biol. 2018 Jul;14(7):706-714. [Content Brief]
Keywords
