NRX-252262

 CAS No.: 2438637-61-5  Cat No.: BP-900076 4.5  

NRX-252262 is an innovative molecular glue that targets the E3 ubiquitin ligase complex, specifically engaging with the CRBN binding site. This small molecule exhibits a unique molecular architecture that facilitates selective protein-protein interactions, leading to targeted protein degradation. The primary mechanism of NRX-252262 involves bridging the interaction between CRBN and its substrate, thereby inducing ubiquitination and subsequent proteasomal degradation of the target protein. This targeted degradation approach is invaluable for research into protein homeostasis and the modulation of protein function. NRX-252262 offers significant potential for elucidating the roles of undruggable proteins and expanding the scope of chemical biology. Its application in degradation studies enables researchers to explore novel biological pathways and mechanisms, providing a powerful tool for dissecting cellular processes at a molecular level. As a cutting-edge reagent, NRX-252262 is poised to advance experimental research, offering a robust platform for the development of next-generation therapeutic strategies targeting previously intractable proteins.

NRX-252262

Structure of 2438637-61-5

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Category
Molecular Glue
Molecular Formula
C23H17Cl2F3N2O4S
Molecular Weight
545.36
Appearance
Solid

* For research and manufacturing use only. Not for human or clinical use.

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Solubility
DMSO: 8.33 mg/mL (15.27 mM; Need ultrasonic)
Appearance
Solid
Storage
Store at -20°C
Mechanism

E3 Ligase: NRX-252262 recruits the cereblon (CRBN) E3 ligase, enabling targeted ubiquitination of specific neosubstrates. The ternary complex formed enhances selective engagement for protein degradation.

Target Protein: NRX-252262 primarily targets IKZF1 and IKZF3 transcription factors, modulating lymphoid cell transcriptional regulation. Binding to these proteins facilitates their recognition by CRBN.

Degradation Mechanism: NRX-252262 induces proteasomal degradation via the ubiquitin–proteasome system. Polyubiquitinated IKZF1/3 is recognized by the 26S proteasome and efficiently cleared from cells.

Applications

• Molecular Glue Mechanism Exploration: NRX-252262 serves as a pivotal tool in elucidating the molecular glue mechanism by promoting selective protein interactions. Researchers can utilize this compound to study how molecular glues facilitate the stabilization of protein-protein interactions, thereby advancing the understanding of targeted protein degradation pathways.

• Targeted Degradation Pathway Analysis: This ligand is instrumental in dissecting targeted degradation pathways. NRX-252262 aids in identifying key molecular interactions that drive the recruitment of E3 ubiquitin ligases, offering insights into the design of novel therapeutics that exploit protein degradation.

• Protein-Protein Interaction Modulation: NRX-252262 provides researchers with a means to modulate protein-protein interactions specifically. By acting as a molecular glue, it enables the study of induced proximity effects, thereby contributing to the development of strategies for targeted protein degradation in various cellular contexts.

• Induced Protein Degradation Studies: Utilizing NRX-252262, scientists can investigate the induced degradation of specific proteins. This compound supports the exploration of how molecular glues can be harnessed to selectively degrade disease-causing proteins, offering potential pathways for therapeutic intervention.

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It is commonly abbreviated as: C1V1 = C2V2

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Tip: Chemical formula is case sensitive. C22H30N4O c22h30n40
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