CAS No.: 2760889-62-9 Cat No.: BP-100173 Purity: ≥95%4.5
Thalidomide-CH2CONH-C2-COOH is a high-purity E3 ligase ligand-linker conjugate specifically designed for PROTAC (Proteolysis Targeting Chimera) research and drug development. This compound features a thalidomide-based CRBN (Cereblon E3 ubiquitin ligase) ligand tethered via a cleavable CH2CONH-linked flexible spacer (C2-COOH), which allows straightforward coupling to target protein binders.
As a core building block in PROTAC design, Thalidomide-CH2CONH-C2-COOH enables the creation of custom bifunctional molecules for targeted protein degradation. Its structure supports efficient recruitment of the CRBN E3 ligase complex, thereby facilitating ubiquitination and subsequent proteasomal degradation of specific target proteins. This product is essential for researchers working on novel PROTACs aimed at oncology, neurodegenerative disease, and other therapeutic areas where targeted protein knockdown is desired.
Structure of 2760889-62-9
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Category
E3 Ligase Ligand-Linker Conjugate
Molecular Formula
C18H18N4O7
Molecular Weight
402.36
* For research and manufacturing use only. Not for human or clinical use.
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Thalidomide-CH2CONH-C2-COOH is a specialized E3 ligase ligand-linker conjugate designed for use in the construction of PROTACs (Proteolysis Targeting Chimeras). It is derived from thalidomide, a well-known ligand for the cereblon (CRBN) E3 ubiquitin ligase. The unique structure of this molecule, featuring a thalidomide moiety joined to a carboxylic acid via a stable linker, facilitates efficient and versatile PROTAC synthesis, enabling targeted protein degradation in both research and drug discovery applications.
Mechanism
Thalidomide-CH2CONH-C2-COOH functions by recruiting the CRBN E3 ubiquitin ligase through the thalidomide ligand component. The linker chain terminates in a carboxyl group, which allows easy conjugation to a target protein ligand (warhead) via amide coupling to create bifunctional molecules. When incorporated into a PROTAC, this conjugate acts by bringing a target protein into proximity with the E3 ligase, triggering ubiquitination and subsequent proteasomal degradation of the target protein. This mechanism provides a powerful alternative to traditional inhibition, offering the ability to eliminate disease-causing proteins from cells.
Applications
Thalidomide-CH2CONH-C2-COOH is widely used in the development of next-generation PROTACs for targeted protein degradation. Its applications include research on degradation of oncogenic or pathogenic proteins, exploration of undruggable targets, and evaluation of new therapeutic approaches in cancer, neurodegenerative diseases, and immunology. The product is ideal for medicinal chemistry workflows, facilitating the synthesis of custom PROTAC molecules and accelerating the lead optimization process in the drug discovery pipeline. It is also valuable for academic research focused on understanding the biology and pharmacology of targeted protein degradation.
• Carboxylic acid functionality enables versatile coupling with target ligands for customizable PROTAC design.
• Thalidomide-based structure specifically recruits CRBN E3 ligase, ensuring efficient and selective target 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
CAS No.: 2760889-62-9
Purity: ≥95%
