Thalidomide 4'-ether-alkylC2-amine hydrochloride is a specialized E3 Ligase Ligand-Linker Conjugate designed for use in PROTAC (Proteolysis Targeting Chimera) drug development. This compound features a thalidomide-based E3 ligase recruiting motif linked via a two-carbon alkylamine linker, making it ideal for assembling bifunctional molecules that harness the ubiquitin-proteasome system. As a building block in the synthesis of PROTACs, Thalidomide 4'-ether-alkylC2-amine hydrochloride facilitates targeted protein degradation by selectively recruiting cereblon (CRBN) E3 ligase to the protein of interest. This product serves as a key intermediate for researchers working to design next-generation therapeutics aimed at previously 'undruggable' targets, offering routes to innovative treatments in oncology, neurology, and immunology. With its high purity and ready-to-use hydrochloride salt form, it ensures robust and reproducible PROTAC assembly for academic and pharmaceutical research.
Structure of 2341840-99-9
* For research and manufacturing use only. Not for human or clinical use.
| Size | Price | Stock | Quantity |
|---|---|---|---|
| 500 mg | $1099 | In stock |
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Background Introduction
Thalidomide 4'-ether-alkylC2-amine hydrochloride is a synthetic small molecule designed as a versatile E3 ligase ligand-linker conjugate. It features a thalidomide core structure, renowned for its cereblon (CRBN) binding properties, linked via a 2-carbon (C2) alkyl chain terminated with an amine hydrochloride group. This optimized structure facilitates its integration into Proteolysis Targeting Chimeras (PROTACs) for targeted protein degradation strategies. As an advanced building block, this molecule enables streamlined assembly of functional PROTACs to selectively manipulate protein homeostasis within cells.
Mechanism
This compound operates by harnessing thalidomide’s ability to bind to the CRBN E3 ubiquitin ligase, a pivotal element in the ubiquitin-proteasome system. The 4'-ether-alkylC2-amine linker allows the thalidomide moiety to be chemically conjugated to a target protein ligand, forming a functional PROTAC molecule. Upon administration, the bifunctional PROTAC brings the protein of interest into close proximity with the CRBN E3 ligase, promoting polyubiquitination and subsequent proteasomal degradation of the target protein. This selective mechanism bypasses the need for traditional enzyme inhibition, offering a powerful route to modulate previously ‘undruggable’ proteins.
Applications
Thalidomide 4'-ether-alkylC2-amine hydrochloride is widely used in the development of next-generation PROTAC molecules and related targeted protein degradation technologies. Its primary applications include the synthesis of bespoke PROTACs for research in cellular biology, drug discovery, and identification of novel therapeutic targets. The compound serves as a modular E3 ligase recruiting handle, facilitating the creation of libraries of protein degraders aimed at oncology, neurodegenerative diseases, immunology, and beyond. As a result, it is a highly valuable tool for academic labs and pharmaceutical R&D focusing on innovative small molecule therapeutics.
* 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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