2243076-67-5
Chemical Structure
ZXH-3-26
- CAS. Nr.: 2243076-67-5
- Formula:C38H37ClN8O7S
- Molecular Weight:785.27
IUPAC Name: methyl 2-((6S)-4-(4-chlorophenyl)-2-((5-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)pentyl)carbamoyl)-3,9-dimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate
InChIKey: OTKOFICOCDRNDA-PMCHYTPCSA-N
SMILES: O=C(OC)C[C@H]1C2=NN=C(C)N2C3=C(C(C)=C(C(NCCCCCNC4=CC=CC(C(N5C(CC6)C(NC6=O)=O)=O)=C4C5=O)=O)S3)C(C7=CC=C(Cl)C=C7)=N1
Biological Activity: ZXH-3-26 is a CRBN-recruiting BRD4 PROTAC degrader with a DC50/5h of approximately 5 nM. ZXH-3-26 drives the ubiquitination and degradation of BRD4 by recruiting BRD4BD1 to the CRL4CRBN E3 ubiquitin ligase complex, thereby inhibiting the dynamic distribution of super-enhancers. ZXH-3-26 reverses TNF-α-induced impairment of the immunosuppressive function of mesenchymal stem cells, and affects RNA synthesis and the transcriptional elongation process of Pol II. ZXH-3-26 can be used in studies related to inflammatory arthritis, malignant tumors, and HIV latency[1][2][3][4][5][6][7].
| Art. -Nr. | Produktname | Reinheit | Beschreibung | Pricing | |||||||||||||||||||
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ZXH-3-26 | 99.53% | ZXH-3-26 is a CRBN-recruiting BRD4 PROTAC degrader with a DC50/5h of approximately 5 nM. ZXH-3-26 drives the ubiquitination and degradation of BRD4 by recruiting BRD4BD1 to the CRL4CRBN E3 ubiquitin ligase complex, thereby inhibiting the dynamic distribution of super-enhancers. ZXH-3-26 reverses TNF-α-induced impairment of the immunosuppressive function of mesenchymal stem cells, and affects RNA synthesis and the transcriptional elongation process of Pol II. ZXH-3-26 can be used in studies related to inflammatory arthritis, malignant tumors, and HIV latency. | ||||||||||||||||||||
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References
- [1]. García Jiménez D, et al. Designing Soluble PROTACs: Strategies and Preliminary Guidelines. Journal of medicinal chemistry. 2022 Oct 13;65(19):12639-12649.
- [2]. 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]
- [3]. Shi Y, et al. BRD4-targeting PROTAC as a unique tool to study biomolecular condensates. Cell Discov. 2023 May 9;9(1):47. [Content Brief]
- [4]. Turner A-MW, et al. BET degraders reveal BRD4 disruption of 7SK and P-TEFb is critical for effective reactivation of latent HIV in CD4+ T-cells. J Virol. 2025 Apr 15;99(4):e0177724.
- [5]. Garcia Jimenez D, et al. IMHB-Mediated Chameleonicity in Drug Design: A Focus on Structurally Related PROTACs. Journal of medicinal chemistry. 2024 Jul 11;67(13):11421-11434.
- [6]. Zhang W, et al. TNF-α-driven m6A modification disrupts the immunoregulatory function of MSCs by regulating HDAC5-dependent super-enhancers. Cell death & disease. 2025 Dec 23;16(1):902.
- [7]. Erdogdu NU, et al. Histone acetylation-dependent clustering of BRD2 instructs transcription dynamics. Nature genetics. 2026 Apr;58(4):854-868. [Content Brief]
