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 a potent and selective BRD4BD1 PROTAC degrader with a DC50 of approximately 500 nM. dBET57 forms a ternary complex with CRL4CRBN and BRD4BD1, induces the ubiquitination and degradation of BRD4, and indirectly inhibits the transcription of MYCN, c-Myc and PD-L1, ultimately leading to cell cycle arrest and apoptosis. dBET57 can be used in related research on neuroblastoma, non-small cell lung cancer and colorectal cancer[1][2][3][4].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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dBET57 | 99.94% | dBET57 is a potent and selective BRD4BD1 PROTAC degrader with a DC50 of approximately 500 nM. dBET57 forms a ternary complex with CRL4CRBN and BRD4BD1, induces the ubiquitination and degradation of BRD4, and indirectly inhibits the transcription of MYCN, c-Myc and PD-L1, ultimately leading to cell cycle arrest and apoptosis. dBET57 can be used in related research on neuroblastoma, non-small cell lung cancer and colorectal cancer. | ||||||||||||||||||||
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References
- [1]. Nowak RP, et al. Plasticity in binding confers selectivity in ligand-induced protein degradation. Nature chemical biology. 2018 Jul;14(7):706-714. [Content Brief]
- [2]. Zhao LP, et al. Carrier-Free Nano-PROTACs to Amplify Photodynamic Therapy Induced DNA Damage through BRD4 Degradation. Nano letters. 2023 Jul 12;23(13):6193-6201.
- [3]. Zhao LP, et al. Chemotherapy-Enabled Colorectal Cancer Immunotherapy of Self-Delivery Nano-PROTACs by Inhibiting Tumor Glycolysis and Avoiding Adaptive Immune Resistance. Advanced science (Weinheim, Baden-Wurttemberg, Germany). 2024 Apr;11(15):e2309204.
- [4]. Jia SQ, et al. The BRD4 Inhibitor dBET57 Exerts Anticancer Effects by Targeting Superenhancer-Related Genes in Neuroblastoma. Journal of immunology research. 2022;2022:7945884. [Content Brief]
