Thalidomide-O-amido-C6-NH2 (TFA) is a specialized E3 Ligase Ligand-Linker Conjugate designed for use in PROTAC (Proteolysis Targeting Chimera) drug development. This compound links a thalidomide-based E3 ligase ligand to a six-carbon amide linker terminating in a primary amine, offering versatile conjugation capabilities for the assembly of custom PROTAC molecules. Thalidomide derivatives are known to recruit the CRBN (Cereblon) E3 ubiquitin ligase, a popular target in targeted protein degradation research. Thalidomide-O-amido-C6-NH2 is ideal for medicinal chemistry applications requiring high purity E3 ligase recruiting elements equipped with functional linkers, supporting the generation of bifunctional molecules that promote target protein ubiquitination and subsequent proteasomal degradation. Perfect for emerging therapeutic strategies and proof-of-concept studies, this conjugate supports a variety of applications in chemical biology and drug discovery focused on harnessing the power of targeted protein degradation.
Structure of 1950635-14-9
* For research and manufacturing use only. Not for human or clinical use.
| Size | Price | Stock | Quantity |
|---|---|---|---|
| 100 mg | $439 | In stock |
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Background Introduction
Thalidomide-O-amido-C6-NH2 (TFA) is a specialized E3 ligase ligand-linker conjugate widely utilized in the development of PROTACs (Proteolysis Targeting Chimeras) for targeted protein degradation. This compound incorporates thalidomide, which serves as a cereblon (CRBN) E3 ubiquitin ligase recruiter, and features a C6 amide linker terminating in a primary amine functional group (NH2), making it ideal for downstream conjugation.
Mechanism
Thalidomide-O-amido-C6-NH2 (TFA) functions as a modular building block in PROTAC synthesis. The thalidomide moiety binds specifically to the CRBN E3 ligase, recruiting the ubiquitination complex to the target protein. The C6 linker provides optimal spatial separation while the terminal amine enables convenient coupling with diverse warheads through standard amide bond formation or other chemical linkages. By bridging an E3 ligase and a protein-targeting warhead, the resulting PROTAC mediates ubiquitination and subsequent degradation of the target protein via the proteasome pathway.
Applications
Thalidomide-O-amido-C6-NH2 (TFA) is extensively used in chemical biology, drug discovery, and targeted protein degradation research. Its primary application is in constructing CRBN-based PROTACs for the study and selective elimination of disease-relevant proteins, such as kinases, transcription factors, and epigenetic regulators. The terminal NH2 functionality allows flexible conjugation to a wide range of ligands, enabling the rapid design and optimization of novel PROTAC molecules. Additionally, this conjugate can be leveraged in the development of molecular glues and other heterobifunctional therapeutics for oncology, neurodegenerative disorders, and immunology.
Hello, can Thalidomide-O-amido-C6-NH2 (TFA) be used for synthesizing PROTAC molecule?
Yes! Thalidomide-O-amido-C6-NH2 (TFA) can be used to synthesize PROTAC molecule.
4/1/2020
Could you describe Thalidomide-O-amido-C6-NH2 (TFA) in detail?
Of course I could. Thalidomide-O-amido-C6-NH2 TFA (Cereblon Ligand-Linker Conjugates 11 TFA) is a synthetic E3 ligand-Linker conjugates, Contains Thalidomide based cereblon ligand and 1 linker.
20/9/2021
synthesize PROTAC molecule
It was used to synthesize PROTAC molecule with a good yield in my experiment, would recommend.
13/1/2017
* 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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