2380000-55-3
Chemical Structure
β-NF-JQ1
- CAS No.: 2380000-55-3
- Formula:C45H42ClN5O6S
- Molecular Weight:816.36
IUPAC Name: (S)-2-(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-((4-(1-oxo-1H-benzo[f]chromen-3-yl)benzyl)oxy)ethoxy)ethoxy)ethyl)acetamide
InChIKey: OZFKLXDOAZGVSV-BHVANESWSA-N
SMILES: O=C(NCCOCCOCCOCC1=CC=C(C2=CC(C3=C(O2)C=CC4=CC=CC=C34)=O)C=C1)C[C@H]5C6=NN=C(C)N6C7=C(C(C)=C(C)S7)C(C8=CC=C(Cl)C=C8)=N5
Biological Activity: β-NF-JQ1 is a BRD2/3/4 PROTAC degrader. β-NF-JQ1 recruits the AhR E3 ligase complex to BRD2, BRD3 and BRD4, induces AhR-BRD interaction, and mediates AhR-dependent degradation through the proximity effect between the target protein and AhR. β-NF-JQ1 acts as an antiproliferative and cytotoxic agent that induces anticancer activity associated with BRD protein knockdown. β-NF-JQ1 can be used for research on breast cancer and neuroblastoma[1][2].
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β-NF-JQ1 | 98.05% | β-NF-JQ1 is a BRD2/3/4 PROTAC degrader. β-NF-JQ1 recruits the AhR E3 ligase complex to BRD2, BRD3 and BRD4, induces AhR-BRD interaction, and mediates AhR-dependent degradation through the proximity effect between the target protein and AhR. β-NF-JQ1 acts as an antiproliferative and cytotoxic agent that induces anticancer activity associated with BRD protein knockdown. β-NF-JQ1 can be used for research on breast cancer and neuroblastoma. | ||||||||||||||||||||
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- [1]. Ohoka N, et al. Development of Small Molecule Chimeras That Recruit AhR E3 Ligase to Target Proteins. ACS chemical biology. 2019 Dec 20;14(12):2822-2832. [Content Brief]
- [2]. Shoda T, et al. Targeted Protein Degradation by Chimeric Compounds using Hydrophobic E3 Ligands and Adamantane Moiety. Pharmaceuticals (Basel, Switzerland). 2020 Feb 25;13(3):34. [Content Brief]
Keywords
