Chemical Name: N1,N20-bis((S)-1-((2S,4R)-4-Hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)-3,6,9,12,15,18-hexaoxaicosanediamide
Biological ActivityHomo-PROTAC for self-degradation of the long form of VHL, pVHL30 (DC50 < 100 nM). Composed of two VHL ligands joined by a linker. Exhibits > 1000-fold increased cellular activity compared to the parent VHL ligand, VH 032. Dimerizes pVHL30 with high avidity in vitro. Induced potent and rapid self-degradation of VHL in cell lines in a highly isoform dependent fashion. Negative control CMP 98 (Cat. No. 6417) also available.
PROTACs are bi-functional small molecules that harness the ubiquitin/proteasome system (UPS) to selectively and catalytically remove target proteins from cells.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation.
Maniaci et al.
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