Carfilzomib is an irreversible proteasome inhibitor and antineoplastic agent that is used in treatment of refractory multiple myeloma. Carfilzomib is associated with a low rate of serum enzyme elevations during treatment and has been implicated to rare instances of clinically apparent, acute liver injury some of which have been fatal.
CAT No: 10-101-326
CAS No:868540-17-4
Synonyms/Alias:N-{(2S)-2-[(Morpholin-4-ylacetyl)aMino]-4-phenylbutanoyl}-L-leucyl-N-{(2S)-4-Methyl-1-[(2R)-2-Methyloxiran-2-yl]-1-oxopentan-2-yl}-L-phenylalaninaMide;CarfilzoMib salt; CarfilzoMib/PR 171; PR 171; PR-171 (CarfilzoMib);(alphaS)-alpha-[(4-Morpholinylacetyl)amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyloxiranyl]carbonyl]butyl]-L-phenylalaninamide; Carfilzomib;
Carfilzomib is a synthetic tetrapeptide epoxyketone that functions as a potent, selective, and irreversible inhibitor of the chymotrypsin-like activity of the 20S proteasome. As a member of the epoxyketone peptide class, it has garnered significant attention in molecular and cellular biology due to its ability to modulate protein degradation pathways, making it a valuable tool for dissecting proteostasis and ubiquitin-proteasome system (UPS) dynamics. Its high specificity and mechanism-based inhibition profile have established it as a critical reagent for investigating proteasome-dependent processes in a variety of in vitro and ex vivo experimental models. The unique biochemical attributes of carfilzomib provide researchers with a means to precisely interrogate the consequences of proteasome inhibition on cellular homeostasis, signaling networks, and protein turnover.
Proteasome inhibition studies: Carfilzomib is extensively utilized in research aimed at understanding the biochemical and cellular consequences of proteasome inhibition. By selectively blocking the chymotrypsin-like activity within the 20S core particle, it enables researchers to dissect the roles of protein degradation in cell cycle regulation, apoptosis, and stress responses. Its irreversible binding mechanism allows for the sustained suppression of proteasomal activity, facilitating time-course experiments and mechanistic studies that require prolonged inhibition without rapid reversibility.
Ubiquitin-proteasome system (UPS) pathway analysis: As a highly specific proteasome inhibitor, carfilzomib is instrumental in elucidating the functional importance of the UPS in protein quality control, signal transduction, and the regulation of transcription factors. Researchers employ it to induce the accumulation of ubiquitinated substrates, thereby uncovering degradation targets, mapping ubiquitination sites, and characterizing the interplay between ubiquitin ligases, deubiquitinases, and proteasomal subunits. Its use supports the development of models for protein misfolding disorders and provides insights into the molecular basis of cellular stress adaptation.
Cellular signaling research: The compound is widely applied in studies investigating the impact of proteasomal blockade on intracellular signaling pathways. By preventing the degradation of short-lived regulatory proteins, carfilzomib facilitates the analysis of signal transduction cascades such as NF-κB, p53, and other pathways modulated by proteasome-dependent turnover. This approach enables the identification of proteasome-regulated nodes within signaling networks, contributing to a deeper understanding of how protein stability influences cellular fate decisions.
Protein homeostasis and quality control investigations: Carfilzomib serves as a valuable reagent in the study of protein homeostasis mechanisms, particularly in the context of endoplasmic reticulum-associated degradation (ERAD) and autophagy-proteasome crosstalk. Its ability to induce proteotoxic stress by inhibiting proteasomal degradation makes it suitable for modeling cellular responses to misfolded or aggregated proteins. Researchers leverage this property to explore compensatory pathways, such as autophagic flux, chaperone upregulation, and the unfolded protein response, thereby advancing knowledge of cellular quality control systems.
Drug discovery and chemical biology: The compound is frequently incorporated into high-throughput screening assays and chemical biology platforms for the identification and characterization of novel modulators of the proteasome or the UPS. Its well-defined inhibitory profile provides a benchmark for evaluating the potency and selectivity of new small molecules, peptides, or biologics targeting proteasomal function. Additionally, carfilzomib is used as a reference compound in structure-activity relationship (SAR) studies, helping to inform the design of next-generation proteasome inhibitors with improved selectivity or pharmacological properties.
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