3094177-94-0
Chemical Structure
U7D-1
- CAS 番号: 3094177-94-0
- Formula:C53H65N9O7
- Molecular Weight:940.14
IUPAC Name: ((1-(benzyloxy)vinyl)oxy)trimethylsilane
InChIKey: BNUWENPJQLIQFO-RTAOZKFSSA-N
SMILES: O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=CC=C3NCCCCCCCCCCCNCC4=CC=C(C5=C(C6=NN5C)N=CN(CC7(O)CCN(C(C[C@H](C8=CC=CC=C8)C)=O)CC7)C6=O)C=C4)=O
Biological Activity: U7D-1 is a USP7 PROTAC degrader that induces selective proteasomal degradation of USP7. U7D-1 destabilizes and downregulates the expression of variant PRC1 complex subunits PCGF1, RING1A and PCGF6, and also slightly reduces the protein level of KDM2B. U7D-1 decreases cell viability, arrests neuroblastoma cells at the G0/G1 cell cycle phase, and downregulates the expression of target genes of PAX3::FOXO1 in FP-RMS cells. U7D-1 increases the level of cleaved PARP in FP-RMS cells, induces cell apoptosis, and upregulates the expression of muscle differentiation markers MYH1 and MYF5. U7D-1 inhibits the growth and proliferation of p53 wild-type and mutant cancer cells, and regulates the apoptosis pathway and E2F pathway. U7D-1 is applicable to studies on neuroblastoma, fusion-positive rhabdomyosarcoma, p53-mutant cancers and cancer-related research[1][2][3][4][5].
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U7D-1 | 99.68% | U7D-1 is a USP7 PROTAC degrader that induces selective proteasomal degradation of USP7. U7D-1 destabilizes and downregulates the expression of variant PRC1 complex subunits PCGF1, RING1A and PCGF6, and also slightly reduces the protein level of KDM2B. U7D-1 decreases cell viability, arrests neuroblastoma cells at the G0/G1 cell cycle phase, and downregulates the expression of target genes of PAX3::FOXO1 in FP-RMS cells. U7D-1 increases the level of cleaved PARP in FP-RMS cells, induces cell apoptosis, and upregulates the expression of muscle differentiation markers MYH1 and MYF5. U7D-1 inhibits the growth and proliferation of p53 wild-type and mutant cancer cells, and regulates the apoptosis pathway and E2F pathway. U7D-1 is applicable to studies on neuroblastoma, fusion-positive rhabdomyosarcoma, p53-mutant cancers and cancer-related research. | ||||||||||||||||||||
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References
- [1]. Cmarik EA, et al. Inhibition of USP7 Destabilizes the Noncanonical PRC1.1 Complex and Induces Neuroblastoma Differentiation. Molecular cancer research : MCR. 2026 Jul 02;24(7):555-575. [Content Brief]
- [2]. Táboas P, et al. USP7 sustains PAX3::FOXO1 enhancer reprogramming and represents a therapeutic vulnerability in Rhabdomyosarcoma. bioRxiv. 2026 Jun 8.
- [3]. Pei Y, et al. Discovery of a Potent and Selective Degrader for USP7. Angewandte Chemie (International ed. in English). 2022 Aug 15;61(33):e202204395. [Content Brief]
- [4]. Dai XJ, et al. Degraders in epigenetic therapy: PROTACs and beyond. Theranostics. 2024;14(4):1464-1499. [Content Brief]
- [5]. Sun D, et al. Blocking Non-enzymatic Functions by PROTAC-Mediated Targeted Protein Degradation. Journal of medicinal chemistry. 2022 Nov 10;65(21):14276-14288. [Content Brief]
