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E3 ligase ligands bind ubiquitin ligases such as cereblon and von Hippel-Lindau (VHL) in degrader design. In a degrader, they anchor the ligase end of the molecule. E3 ubiquitin ligases transfer ubiquitin to substrate proteins and mark them for degradation by the proteasome. Thalidomide and its analogs bind cereblon (CRBN), a substrate receptor of a cullin-based E3 ligase complex identified as their direct target in 2010. The category includes cereblon ligands such as thalidomide fluoride and TD-106, and VHL ligands such as VL285 and VH032-cyclopropane-F. These ligands are used to build proteolysis-targeting chimeras (PROTACs) and to study how ligases are recruited to new substrates.
TD-106 is a cereblon (CRBN) modulator, which can be used for targeted protein degradation. BRD4 PROTACs with TD-106 induce BRD4 degradation.
CC-885 is a cereblon (CRBN) modulator with potent anti-tumour activity.
Iberdomide (CC-220) is a cereblon (CRBN) modulator with an IC50 of 60 nM.
CRBN modulator-1, a Thalidomide analog and a CRBN modulator extracted from WO2020006262A1, compound 10, has an IC50 of 3.5 μM and a Ki of 0.98 μM.
Synonyms: CC-90009
Eragidomide is a selective cereblon (CRBN) E3 ligase modulator that acts as a molecular glue, specifically targeting GSPT1 for ubiquitination. By co-opting the CRL4CRBN complex, Eragidomide facilitates the proteasomal degradation of GSPT1, leading to significant biological effects. This compound is primarily utilized in research applications focused on cancer biology and therapeutic strategies that exploit the proteasome pathway.
AG6033 is a novel modulator of the cereblon (CRBN) protein. This compound effectively suppresses various tumor cell lines by influencing the interactions between CRBN and key antitumor target proteins, leading to the degradation of GSPT1 and IKZF1. AG6033 has demonstrated a CRBN-dependent cytotoxic effect, making it a valuable tool for research in cancer biology and the development of targeted therapies.
Synonyms: CC-99282
Golcadomide is a potent modulator of the CRBN E3 ligase, functioning as a CELMoD that promotes the ubiquitin-mediated proteasomal degradation of key transcription factors such as Ikaros and Aiolos through its interaction with the CRL4 CRBN substrate receptor. This compound has significant biological activity in cancer research, particularly in the study of chronic lymphocytic leukemia (CLL) and non-Hodgkin lymphoma (NHL). Golcadomide's unique mechanism positions it as a valuable tool for exploring therapeutic pathways in hematological malignancies.
CC-3060 is a Cereblon modulator that facilitates the degradation of ZBTB16, showing a DC50 value of 0.47 nM in HT-1080 cells. This compound engages specific structural degrons across various zinc finger domains, effectively promoting ZBTB16's proteasomal degradation. CC-3060 has potential applications in the study of cellular processes regulated by ZBTB16 and in the development of innovative therapeutic strategies targeting this pathway.
Cereblon inhibitor 1 is an isoindoline derivative that functions as a modulator of cereblon E3 ubiquitin ligase. This compound is designed to inhibit cerablon activity, making it a valuable tool for cancer research by disrupting protein homeostasis and influencing cell signaling pathways. Its application may extend to studying the therapeutic potential of targeting E3 ligases in various cancer models.
ZXH-1-161 is a selective modulator of cereblon (CRBN) that induces the degradation of GSPT1 in a CRBN-dependent manner. This compound effectively inhibits the proliferation of multiple myeloma cells and demonstrates significant antitumor activity. Its unique mechanism of action makes it a valuable tool for investigating CRBN-targeted therapies in cancer research.
