Thalidomide-O-amido-C8-NH2 (TFA) is a premium E3 Ligase Ligand-Linker Conjugate specifically designed for use in PROTAC (Proteolysis Targeting Chimera) drug development. This compound integrates the cereblon (CRBN) ligand thalidomide with a C8 amide-based linker, terminating in a primary amine (NH2), all provided as a trifluoroacetate (TFA) salt. Thalidomide-O-amido-C8-NH2 enables researchers to create highly effective PROTAC molecules by facilitating the recruitment of the CRBN E3 ubiquitin ligase, a crucial step in targeted protein degradation. As a critical tool in the synthesis of next-generation therapeutics, this conjugate supports rapid assembly of PROTACs directed toward challenging disease-related proteins, accelerating drug discovery in oncology, neurodegeneration, and other therapeutic areas. Ideal for medicinal chemistry labs and pharmaceutical R&D, Thalidomide-O-amido-C8-NH2 (TFA) ensures high purity and robust performance in advanced protein degradation research.
Structure of 1950635-16-1
* For research and manufacturing use only. Not for human or clinical use.
| Size | Price | Stock | Quantity |
|---|---|---|---|
| 100 mg | $469 | In stock |
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Background Introduction
Thalidomide-O-amido-C8-NH2 (TFA) is a specialized E3 ligase ligand-linker conjugate, frequently used in the research and development of PROTACs (Proteolysis Targeting Chimeras). Serving as a thalidomide-based cereblon (CRBN) ligand functionalized with an eight-carbon linker ending in a primary amine, this compound offers versatile conjugation possibilities for generating targeted protein degraders. The TFA salt form enhances its solubility and stability, making it suitable for various medicinal chemistry and chemical biology applications.
Mechanism
Thalidomide-O-amido-C8-NH2 (TFA) acts as a bifunctional building block, designed to recruit the E3 ubiquitin ligase cereblon (CRBN) within PROTAC constructs. The thalidomide moiety binds specifically to CRBN, while the C8 amido linker provides optimal spacing and flexibility for attaching diverse target protein ligands through the terminal amine group. Once tethered to a ligand for the protein of interest, the resulting PROTAC can induce proximity-driven ubiquitination and subsequent proteasomal degradation of the target protein, thereby facilitating selective and catalytic protein knockdown.
Applications
Thalidomide-O-amido-C8-NH2 (TFA) is widely used in the design, synthesis, and optimization of PROTACs for targeted protein degradation studies. Its extended amide linker and reactive primary amine enable customizable conjugations with various warheads or payloads, allowing researchers to tailor PROTACs for different targets. Key applications include exploratory drug discovery, mechanistic studies on protein homeostasis, and functional validation of potential therapeutic protein targets in oncology, immunology, and neurodegenerative research. The compound’s utility also extends to generating molecular glues, studying E3 ligase biology, and developing novel therapeutic modalities in the field of targeted protein degradation.
* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C1V1 = C2V2
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