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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.
PROTAC CRBN Degrader-1 comprises a cereblon (CRBN) ligand binding group, a linker and an von Hippel-Landau (VHL) binding group. PROTAC CRBN Degrader-1 is an cereblon (CRBN) degrader.
Homo-PROTAC cereblon degrader 1 (compound 15a) is a highly potent and efficient cereblon (CRBN) degrader with only minimal effects on IKZF1 and IKZF3.
BI-3663 is a highly selective PTK2/FAK PROTAC, with cereblon ligands to hijack E3 ligases for PTK2 degradation. BI-3663 inhibits PTK2 with an IC50 of 18 nM. BI-3663 is a PROTAC that composes of BI-4464 linked to Pomalidomide with a linker. Anti-cancer activity.
Synonyms: MDK7526; Protein degrader 1; VHL Ligand 1; ULM-1; VH032 desacetyl; VH032 amine; Degradation Inducing Moiety A
(S,R,S)-AHPC , also known as also known as MDK7526; VHL Ligand 1; Protein degrader 1, is a potent and selective protein degrader. MDK7526 is potential useful for the targeted degradation of the androgen receptor.
CRBN-6-5-5-VHL is a potent and selective VHL-based PROTAC degrader targeting cereblon (CRBN), with a DC₅₀ of 1.5 nM. It selectively degrades CRBN without affecting neo-substrates IKZF1 and IKZF3.
TD-165 is a PROTAC (proteolysis-targeting chimera) that targets cereblon (CRBN) for selective degradation of proteins. This compound features a CRBN ligand binding group, a linker, and a von Hippel-Landau (VHL) binding group, facilitating targeted ubiquitination and proteolytic degradation of specific proteins involved in cellular processes. TD-165 is suitable for research applications focused on targeted protein degradation, therapeutic development, and elucidating protein function in various biological contexts.
Thalidomide-5-propargyl is a propargyl-modified derivative of Thalidomide that selectively targets Cereblon (CRBN). By recruiting CRBN proteins, this compound plays a significant role in the development of proteolysis-targeting chimeras (PROTACs). The presence of an alkynyl group enables its direct use in triazole synthesis, facilitating the creation of innovative PROTAC molecules designed for therapeutic applications.
WDR5 Degrader-1 is a cereblon (CRBN)-recruiting compound designed to selectively induce degradation of the WDR5 protein. This degrader effectively targets WDR5 while sparing the CRBN neo-substrate IKZF1, facilitating precise manipulation of WDR5 levels in cellular systems. It is a valuable tool for investigating the biological roles of WDR5 in transcriptional regulation and potential therapeutic strategies in diseases associated with dysregulated WDR5 expression.
IPS-06061 is a molecular glue degrader that targets the KRAS G12D mutant through the formation of a ternary complex with CRBN. This compound effectively degrades KRAS G12D with a DC50 value of less than 500 nM, demonstrating significant anti-tumor efficacy. It serves as a valuable tool for research into targeted therapies for cancers driven by KRAS mutations.
CDLI-5 is a cereblon (CRBN) degrader-linker conjugate designed for the synthesis of cereblon degrader antibody conjugates (cDACs). This compound enables targeted protein degradation through the recruitment of E3 ligases to specific substrates, facilitating effective modulation of protein levels. CDLI-5 serves as a valuable tool in research applications focused on targeted therapies and the development of novel anticancer strategies.
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ALV2 is a potent and selective Helios degrader that functions as a molecular glue. It exhibits an IC50 of 0.57 μM for binding to cereblon (CRBN). By targeting Helios, a zinc-finger transcription factor, ALV2 plays a crucial role in regulating the stability of Treg cell phenotype within the inflammatory tumor microenvironment, making it valuable for research in immunology and cancer therapy.
Synonyms: JBP
5-Norbornene-2-methylamine is a hydrophobic tag utilized in the synthesis of targeted protein degraders. As an E3 ligase ligand, it facilitates the construction of PROTAC molecules, including PROTAC PARP1 degrader-4. This compound is essential for advancing research in protein degradation and its applications in therapeutic development.
3-(6-Amino-1-oxoisoindolin-2-yl)piperidine-2,6-dione is an analog of Lenalidomide that functions by recruiting the cereblon (CRBN) protein. This compound is primarily utilized in PROTAC (Proteolysis Targeting Chimera) research, enabling targeted degradation of specific proteins to elucidate their biological roles and potential therapeutic avenues. Its unique structure and mechanism make it a valuable tool for advancing studies in drug discovery and targeted therapies.
3-(6-Bromo-1-oxoisoindolin-2-yl)piperidine-2,6-dione functions as a Lenalidomide analog with potential utility in targeted protein degradation research. This compound exhibits properties that may facilitate the design of proteolysis-targeting chimeras (PROTACs), thereby enabling the selective degradation of proteins of interest. Further investigation into its biological activity could contribute to advancements in therapeutic strategies aimed at modulating cellular proteostasis and addressing various diseases.
Synonyms: (S,S,S)-VH032-Boc
(S,S,S)-AHPC-Boc is a stereoisomer of (S,R,S)-AHPC-Boc and serves as a valuable experimental control in research. This compound specifically relates to the recruitment of the von Hippel-Lindau (VHL) protein, which plays a critical role in targeted protein degradation through PROTAC technology. By providing a reliable reference point, (S,S,S)-AHPC-Boc facilitates investigations into the efficacy and selectivity of VHL ligands in cellular systems.
Thalidomide acid is a Thalidomide analog that primarily functions as a target for Proteolysis Targeting Chimeras (PROTACs). It exhibits significant activity in modulating protein degradation and is utilized in chemical biology studies aimed at elucidating proteostasis and targeted therapeutics. This compound serves as a valuable tool in drug discovery and development, particularly for diseases related to dysregulated protein levels.
2-(2,6-Dioxopiperidin-3-yl)-5-ethynylisoindoline-1,3-dione is a Thalidomide analog primarily engaged in protein degradation pathways through PROTAC technology. Exhibiting modulatory effects on the immune system and anti-angiogenic properties, this compound is instrumental in investigational studies targeting multiple myeloma and other malignancies. Its distinctive structural attributes facilitate the exploration of targeted therapies and the development of innovative drug delivery platforms.
3-(7-Amino-1-oxoisoindolin-2-yl)piperidine-2,6-dione is a Lenalidomide analog that serves as a valuable tool in PROTAC research. This compound selectively modulates protein degradation pathways, making it instrumental in the development of targeted therapeutics. Its structural similarity to Lenalidomide allows for the exploration of novel therapeutic applications in oncology and immunology.
3-(7-Bromo-1-oxoisoindolin-2-yl)piperidine-2,6-dione is a Lenalidomide analog targeting the ubiquitin-proteasome system. This compound exhibits notable biological activity in the development of PROTACs (proteolysis-targeting chimeras), providing a valuable tool for research into targeted protein degradation. Its structural features enhance the potential for therapeutic applications in oncology and related fields.
Thalidomide-1-Me-5-NH2 is an aminated analog of Thalidomide, primarily targeting E3 ligase activation. This compound serves as a useful intermediate for the development of PROTAC (Proteolysis Targeting Chimera) molecules through amine derivatization. Researchers can utilize this reagent in studies focused on targeted protein degradation and related therapeutic applications.
Deoxy-thalidomide-5-iodine is a Thalidomide analog that serves as a valuable tool in PROTAC (Proteolysis Targeting Chimeras) research. This compound is designed to facilitate targeted protein degradation by recruiting E3 ligases, enabling the selective elimination of specific proteins within cellular systems. Its unique structural modifications may enhance potency and efficacy in various biological assays, making it essential for advancing studies in targeted oncology and therapeutic interventions.
Synonyms: CC-5013 hydrochloride
Lenalidomide hydrochloride is an oral immunomodulatory agent targeting cereblon (CRBN), acting as a molecular glue. It promotes the selective ubiquitination and degradation of transcription factors IKZF1 and IKZF3 via the CRBN-CRL4 ubiquitin ligase complex. This mechanism effectively inhibits the growth of mature B-cell lymphomas, including multiple myeloma, while also inducing the release of IL-2 from T cells, making it valuable in cancer research and therapeutic applications.
VHL Ligand 39 is a conjugate of the VHL E3 ligase, acting as a pivotal intermediate in the construction of PROTAC (proteolysis-targeting chimera) molecules. This compound facilitates targeted protein degradation by harnessing the ubiquitin-proteasome system, enabling researchers to modulate protein levels for various biological studies. Its applications extend to investigating cellular signaling pathways and therapeutic mechanisms involving targeted degradation of specific proteins.
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DA-PROTAC is a selective PROTAC degrader targeting the copper ion-transport proteins Atox1 and CCS. By facilitating the recruitment of E3 ligase, DA-PROTAC promotes the ubiquitination and subsequent proteasomal degradation of both Atox1 and CCS. This compound is particularly valuable for research in triple negative breast cancer, allowing for the investigation of copper transport mechanisms and their implications in tumor biology.
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3-Azathalidomide is a Thalidomide analog that primarily targets the E3 ubiquitin ligase, making it a valuable tool in protein degradation studies. This compound exhibits biological activity that facilitates the development of PROTACs (proteolysis-targeting chimeras), enabling targeted protein degradation in various cellular contexts. Its application is particularly relevant in drug discovery and targeted therapeutics research, where modulation of protein levels is essential for understanding disease mechanisms and therapeutic interventions.
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