2362575-45-7
Chemical Structure
CRBN-6-5-5-VHL
- CAS No.: 2362575-45-7
- Formula:C51H69N7O10S
- Molecular Weight:972.20
IUPAC Name: (2S,4R)-1-((2S)-2-(5-((5-((6-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)hexyl)oxy)pentyl)oxy)pentanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
InChIKey: LIMCHOLAKDUZDS-XARBDFOFSA-N
SMILES: O=C(N1C(CCC2=O)C(N2)=O)C(C(C1=O)=CC=C3)=C3NCCCCCCOCCCCCOCCCCC(N[C@@H](C(C)(C)C)C(N(C[C@@H]4O)[C@@H](C4)C(NCC5=CC=C(C(SC=N6)=C6C)C=C5)=O)=O)=O
Biological Activity: CRBN-6-5-5-VHL is a potent and selective VHL E3 ligand-based Cereblon (CRBN) PROTAC degrader with a DC50 value of 1.5 nM. CRBN-6-5-5-VHL forms a heterotrimeric complex with CRBN and VHL E3 ligase, thereby promoting CRBN ubiquitination and proteasomal degradation without inducing VHL degradation. CRBN-6-5-5-VHL protects myeloma from the toxic effects of IMiDs. CRBN-6-5-5-VHL can be used in the research of multiple myeloma[1][2][3][4].
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CRBN-6-5-5-VHL | 98.97% | CRBN-6-5-5-VHL is a potent and selective VHL E3 ligand-based Cereblon (CRBN) PROTAC degrader with a DC50 value of 1.5 nM. CRBN-6-5-5-VHL forms a heterotrimeric complex with CRBN and VHL E3 ligase, thereby promoting CRBN ubiquitination and proteasomal degradation without inducing VHL degradation. CRBN-6-5-5-VHL protects myeloma from the toxic effects of IMiDs. CRBN-6-5-5-VHL can be used in the research of multiple myeloma. | ||||||||||||||||||||
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- [1]. Steinebach C, et al. PROTAC-mediated crosstalk between E3 ligases. Chemical communications (Cambridge, England). 2019 Feb 05;55(12):1821-1824. [Content Brief]
- [2]. Kuwahara-Ota S, et al. Lenalidomide and pomalidomide potently interfere with induction of myeloid-derived suppressor cells in multiple myeloma. British journal of haematology. 2020 Dec;191(5):784-795. [Content Brief]
- [3]. Konstantinidou M, et al. PROTACs- a game-changing technology. Expert opinion on drug discovery. 2019 Dec;14(12):1255-1268. [Content Brief]
- [4]. Essa K, et al. Leveraging Targeted Protein Degradation for G Protein-Coupled Receptors: The Development of CCR2 Molecular Degraders. Journal of medicinal chemistry. 2025 Dec 25;68(24):26525-26546. [Content Brief]
Keywords
