CAS No.: 1957236-36-0 Cat No.: BP-100163 Purity: ≥95%4.5
Pomalidomide-C8-NH2 is a high-purity E3 Ligase Ligand-Linker Conjugate specifically designed for use in PROTAC (Proteolysis Targeting Chimera) drug development. This compound consists of the immunomodulatory agent pomalidomide, a well-characterized CRBN (Cereblon) E3 ubiquitin ligase binder, connected via an octyl (C8) alkyl linker terminating with a primary amine (NH2) group. Pomalidomide-C8-NH2 serves as an efficient intermediate for custom synthesis of PROTAC molecules, enabling the recruitment of CRBN to induce targeted degradation of disease-relevant proteins. This conjugate is ideal for researchers developing next-generation protein degraders and exploring targeted protein knockdown in oncology, immunology, and neurodegenerative disease models. Pomalidomide-C8-NH2 exemplifies the latest advancements in the category of E3 Ligase Ligand-Linker Conjugates, facilitating innovation in small molecule drug discovery platforms.
Structure of 1957236-36-0
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Category
E3 Ligase Ligand-Linker Conjugate
Molecular Formula
C21H28N4O4
Molecular Weight
400.47
* For research and manufacturing use only. Not for human or clinical use.
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Pomalidomide-C8-NH2 is a specialized E3 ligase ligand-linker conjugate, designed as a key intermediate for the synthesis of PROTACs (Proteolysis Targeting Chimeras) and other targeted protein degradation agents. By incorporating the well-characterized CRBN (cereblon) ligand pomalidomide and a flexible C8 alkyl linker terminating in a primary amine, this compound facilitates modular addition of target protein-binding warheads, streamlining the development of next-generation therapeutics.
Mechanism
Pomalidomide-C8-NH2 functions by acting as a small molecule recruiter of the cereblon (CRBN) E3 ubiquitin ligase complex via its pomalidomide moiety. The attached C8 linker provides optimal spatial separation, and the terminal amine group enables chemical conjugation to diverse target ligands or functional groups. When integrated into a PROTAC construct, this bifunctional molecule brings the E3 ligase and a target protein into proximity, triggering ubiquitination and subsequent proteasomal degradation of the intended protein target.
Applications
Pomalidomide-C8-NH2 is ideal for use in the synthesis and optimization of PROTACs, enabling researchers to selectively degrade pathogenic or otherwise challenging proteins in cellular and in vivo systems. It is widely employed in drug discovery projects for the interrogation of protein function, target validation, and the development of therapeutic degradation agents. The free amine functionality on the C8 linker offers versatile conjugation options for medicinal chemistry, making it a preferred choice for those designing custom PROTACs and targeted protein degradation tools in oncology, neurodegeneration, and immunology research.
• Extended C8 linker increases molecular flexibility, improving target protein accessibility in PROTAC design.
• Amine-terminated structure facilitates efficient conjugation with diverse warheads for customizable CRBN-recruiting PROTAC synthesis.
* 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.: 1957236-36-0
Purity: ≥95%
