Pomalidomide-C2-NH2 is a functionalized derivative of the immunomodulatory drug pomalidomide, specifically engineered for use in PROTAC (Proteolysis Targeting Chimera) and molecular glue research. Featuring a two-carbon linker with a terminal amine group, this E3 ligase ligand facilitates efficient conjugation to target ligands, enabling the design and synthesis of cereblon (CRBN)-recruiting protein degraders. Pomalidomide-C2-NH2 plays a critical role in targeted protein degradation strategies by promoting the ubiquitination and subsequent proteasomal degradation of disease-related proteins. Its application accelerates the development of next-generation therapeutics in oncology, immunology, and other fields that benefit from targeted protein knockdown.
Structure of 1957235-66-3
* For research and manufacturing use only. Not for human or clinical use.
| Size | Price | Stock | Quantity |
|---|---|---|---|
| 25 mg | $199 | In stock | |
| 100 mg | $523 | In stock |
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Background Introduction
Pomalidomide-C2-NH2 is a functionalized derivative of pomalidomide, one of the potent immunomodulatory imide drugs (IMiDs) widely used as a cereblon (CRBN) E3 ligase ligand in targeted protein degradation research. The inclusion of a C2 (two-carbon) amino linker at the imide moiety endows this molecule with increased chemical reactivity and synthetic flexibility, facilitating its use as a building block for PROTAC (Proteolysis Targeting Chimera) and other heterobifunctional degrader constructs. Such modifications are vital for tuning the physicochemical properties and biological compatibility of degrader molecules.
Mechanism
Pomalidomide-C2-NH2 functions by specifically binding to the cereblon (CRBN) component of the CRL4-CRBN E3 ubiquitin ligase complex. In the context of PROTAC chemistry, the exposed C2-amino linker provides an accessible conjugation point for attaching a variety of target protein ligands via amide bond formation or other coupling reactions. Once successfully tethered to a target-ligand motif, the resulting PROTAC molecule can simultaneously engage both CRBN and the protein of interest, thereby facilitating the recruitment of the ubiquitin-proteasome system to polyubiquitinate and degrade the target protein within cells.
Applications
Pomalidomide-C2-NH2 is ideal for drug discovery scientists and medicinal chemists focusing on the design and synthesis of CRBN-based PROTACs, molecular glues, and other heterobifunctional degraders. Its primary applications include:
• Serving as an E3 ligase binding moiety in the construction of CRBN-recruiting PROTACsBy providing a chemically versatile handle, Pomalidomide-C2-NH2 accelerates innovation in targeted protein degradation and supports the rapid prototyping of next-generation degrader therapeutics.
Can you tell me the special storage conditions of Pomalidomide-C2-NH2?
Yes, I can. Keep in dark place, Inert atmosphere, Room temperature.
6/2/2016
Can you give me some information about the structure of Pomalidomide-C2-NH2
Pomalidomide-C2-NH2 is a synthetic E3 ligand linker conjugate containing Pomalidomide-based cereblon ligand and a linker.
2/4/2019
E3 ligase ligand-linker conjugate containing a Pomalidomide-based cereblon ligand
We used Pomalidomide-C2-NH2 as a synthesized E3 ligase ligand-linker conjugate containing a Pomalidomide-based cereblon ligand and a linker in my experiment, it worked well.
3/3/2019
* 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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