E3 ligase Ligand-Linker Conjugates 9 (Synonyms: VH032-PEG6-C4-Cl; VHL Ligand-Linker Conjugates 10; E3 ligase Ligand-Linker Conjugates 9) |
| Catalog No.GC32976 |
E3 ligase Ligand-Linker Conjugates 9 is a conjugate of ligands for E3 and 25-atom-length linker. The connector of linker is Halogen group. E3 ligase Ligand-Linker Conjugates 9 incorporates the (S,R,S)-AHPC based VHL ligand and 6-unit PEG linker. E3 ligase Ligand-Linker Conjugates 9 is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.
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Cas No.: 1835705-59-3
Sample solution is provided at 25 µL, 10mM.
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E3 ligase Ligand-Linker Conjugates 9 is a synthesized compound that incorporates an E3 ligase ligand and a linker used in PROTAC technology.
E3 ligase Ligand-Linker Conjugates 9 uses the VHL ligand[1]. The linker is 6-2-2-2-2-2-2. The linkers contain a mixture of hydrophobic and hydrophilic moieties to balance the hydrophobicity/hydrophilicity of the resulting hybrid compounds. PROTACs that induce the degradation of an oncogenic tyrosine kinase, BCR-ABL has been developed. E3 ligase Ligand-Linker Conjugates 9 can be attached to potent TKIs (bosutinib and dasatinib) that mediate the degradation of c-ABL and BCR-ABL by hijacking either CRBN or VHL E3 ubiquitin ligase [2].
[1]. US 20170121321 A1 [2]. Lai AC, et al. Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL. Angew Chem Int Ed Engl. 2016 Jan 11;55(2):807-10.
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