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E3 ligase Ligand 4 (Thalidomide 4-fluoride) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein, it can connect to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1.
| Molecular Weight | 276.22 |
| Formula | C13H9FN2O4 |
| CAS Number | 835616-60-9 |
| Solubility (25°C) | DMSO ≥ 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Mikołaj Słabicki, et al. Small-molecule-induced polymerization triggers degradation of BCL6
[3] Takumi Ito, et al. Molecular mechanisms of thalidomide and its derivatives
[4] Jun Araya, et al. PRKN-regulated mitophagy and cellular senescence during COPD pathogenesis
| Related Ligand for E3 Ligase Products |
|---|
| Pomalidomide
Pomalidomide is the third-generation immunomodulatory agent, functions through interacting with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors. Pomalidomide is a second generation immunomodulator, TNF-α inhibitor with IC50 of 13 nM. |
| Thalidomide
Thalidomide is a sedative and immunomodulator used to study the symptoms of many cancers, it has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ∼250 nM. |
| VH-298
VH-298 is a potent VHL inhibitor that stabilizes HIF-α and elicits a hypoxic response via a different mechanism, with a Kd value of 80 to 90 nM. |
| VHL Ligand 1 hydrochloride
VHL Ligand 1 hydrochloride is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. |
| E3 ligase Ligand 1
E3 ligase Ligand 1 (VHL ligand 2 hydrochloride; (S,R,S)-AHPC-Me hydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. |
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