Pomalidomide-C2-NH2 (hydrochloride)

Background Introduction

Pomalidomide is a next-generation immunomodulatory imide drug (IMiD) structurally related to thalidomide and lenalidomide, renowned for its improved potency and reduced off-target effects. As a high-affinity ligand for Cereblon (CRBN), an E3 ubiquitin ligase, pomalidomide is a popular choice in targeted protein degradation research. Pomalidomide-C2-NH2 (hydrochloride) is a pomalidomide derivative featuring a two-carbon (C2) amino linker, which offers enhanced versatility for conjugation and synthetic construction of PROTAC (Proteolysis Targeting Chimera) molecules.

Mechanism

Pomalidomide-C2-NH2 (hydrochloride) selectively binds to the CRBN substrate adaptor of the CUL4-CRBN E3 ubiquitin ligase complex. By linking this ligand to a molecule that binds a protein of interest, it acts as a PROTAC E3 ligase recruiter, facilitating the proximity-induced ubiquitination and subsequent proteasomal degradation of the target protein. The C2-amino linker provides a chemically accessible site for further modification, allowing seamless incorporation into larger bifunctional PROTACs with optimized pharmacokinetics and cellular activity.

Applications

Pomalidomide-C2-NH2 (hydrochloride) is widely employed in the design and synthesis of CRBN-based PROTACs and molecular glues for targeted protein degradation. The compound's C2-amino linker supports strategic conjugation with various ligands, enabling rapid exploration of structure-activity relationships (SAR) and fine-tuning of degrader properties. Researchers utilize this E3 ligase ligand for:

• Assembly of customized CRBN-targeting PROTAC libraries
• Development of molecular glue degraders for previously undruggable targets
• Drug discovery, validation of new therapeutic targets, and chemical biology studies
• Academic and contract research for innovative TPD (targeted protein degradation) platforms

• High-purity compound verified by HPLC, NMR, and LC-MS
• Consistent batch-to-batch reproducibility with complete QC documentation
• Supplied with COA, MSDS, and analytical data for traceability
• Reliable global shipping with stability-guaranteed packaging
• Dedicated technical support and optional custom synthesis service
• Demonstrates strong binding affinity to CRBN, VHL, or other E3 ligases
• Enables stable E3 ligase recruitment for targeted protein degradation
• Amino-functionalized C2 linker provides versatile conjugation sites for PROTAC assembly.
• High affinity for CRBN E3 ligase enables efficient target protein ubiquitination in PROTAC research.