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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.
Synonyms: Cereblon ligand 4; E3 ligase Ligand 4
Thalidomide fluoride (Cereblon ligand 4) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide fluoride (Cereblon ligand 4) can be connected to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1.
Synonyms: VHL ligand 3; E3 ligase Ligand 19
VH032-cyclopropane-F is the VH032-based VHL ligand. VH032-cyclopropane-F can be connected to the ligand for protein (e.g., SMARCA BD ligand) by a linker to form PROTACs (e.g., PROTAC 1).
E3 ligase Ligand 14 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 14 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
E3 ligase Ligand 10 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 10 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
E3 ligase Ligand 9 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 9 can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs.
Synonyms: VHL ligand 2; E3 ligase Ligand 1A
(S,R,S)-AHPC-Me (VHL ligand 2) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader.
Synonyms: PROTAC IAP binding moiety 2
MV-1-NH-Me, the MV-1 based IAP ligand, binds to ABL inhibitor via a linker to form SNIPER.
Synonyms: PROTAC IAP binding moiety 1
Bestatin-amido-Me, the Bestatin-based IAP ligand, binds to ABL inhibitor via a linker to form SNIPER.
Synonyms: VHL ligand 6
VH032 thiol (VHL ligand 6) is a VHL ligand, which binds to pan-BET inhibitor JQ1 via a linker to form PROTAC.
Synonyms: Cereblon ligand 3; E3 ligase Ligand 3
Thalidomide-O-COOH (Cereblon ligand 3) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein.
Synonyms: Cereblon ligand 2; E3 ligase Ligand 2
Thalidomide-OH (Cereblon ligand 2) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-OH (Cereblon ligand 2) can be connected to the ligand for protein by a linker to form PROTACs.
E3 ligase Ligand 8 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 8 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
Synonyms: VHL ligand 2 hydrochloride; E3 ligase Ligand 1
(S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein.
Synonyms: MDK7526 hydrochloride; MDK 7526; VH032-NH2 hydrochloride; VHL ligand 1 hydrochloride
(S,R,S)-AHPC hydrochloride (MDK7526 hydrochloride) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein.
Tz-Thalidomide is a tetrazine-tagged thalidomide derivative that functions as a ligand for E3 ligases. It exhibits binding affinity for BRD4, with IC₅₀ values of 46.25 μM for BRD4-1 and 62.55 μM for BRD4-2. As a click chemistry reagent, Tz-Thalidomide contains a tetrazine moiety capable of undergoing inverse electron demand Diels–Alder (iEDDA) reactions with trans-cyclooctene (TCO)-containing molecules, enabling bioorthogonal labeling and conjugation applications.
Thalidomide 5-fluoride is a thalidomide-derived ligand for the E3 ubiquitin ligase Cereblon, enabling targeted protein degradation via the PROTAC approach. This compound can be conjugated with specific target protein ligands, such as IRAK4, to create PROTAC molecules for enhanced therapeutic applications. Notably, PROTAC IRAK4 degrader-1 demonstrated significant IRAK4 protein degradation in OCI-LY-10 cells at concentrations of 0.01, 0.1, and 1 μM, achieving degradation levels of 20-50%, and >50%, respectively. This underlines its potential utility in cellular studies of protein regulation and targeted therapeutics.
Thalidomide-5-OH is an E3 ligase ligand that specifically targets the cereblon (CRBN) protein. This compound facilitates the recruitment of CRBN, enabling targeted protein degradation through the formation of PROTACs (proteolysis-targeting chimeras) by linking it to another ligand. Thalidomide-5-OH is utilized in research applications focusing on targeted protein degradation and therapeutic development for various diseases.
Thalidomide-NH-CH2-COOH is a Thalidomide-derived ligand that specifically targets the cereblon (CRBN) protein, facilitating its recruitment in various biological processes. This compound serves as a crucial building block for the development of PROTACs, allowing researchers to design targeted protein degradation strategies. Its application is significant in the study of protein homeostasis and the therapeutic potential of targeted protein modulation.
Thalidomide-propargyl is a thalidomide-derived ligand that selectively targets Cereblon (CRBN) for protein recruitment. This compound is instrumental in the development of immunomodulatory drug (IMiD) based PROTACs, facilitating targeted protein degradation. Additionally, Thalidomide-propargyl features an alkyne functional group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions with azide-containing molecules, making it a valuable tool for click chemistry applications in chemical biology research.
Thalidomide-5,6-F is a Thalidomide-derived ligand that selectively targets cereblon (CRBN), facilitating its recruitment for the targeted degradation of specific proteins via the ubiquitin-proteasome pathway. This compound is instrumental in the development of PROTACs (proteolysis-targeting chimeras), enabling innovative approaches in the research of targeted protein degradation, drug discovery, and therapeutic interventions. Its unique mechanism offers valuable insights into cellular regulation and disease processes.
Thalidomide-5-COOH serves as a ligand for cereblon (CRBN), functioning through its interaction with the E3 ubiquitin ligase complex. This compound is instrumental in the development of PROTACs, enabling targeted protein degradation for potential therapeutic applications. Its role in bridging target proteins for ubiquitination makes it a valuable reagent in chemical biology and drug discovery research.
Thalidomide-O-C8-COOH is a Thalidomide-derived ligand targeting the E3 ligase Cereblon (CRBN). This compound facilitates the recruitment of CRBN protein, serving as a vital component for the development of Proteolysis Targeting Chimeras (PROTACs). Its unique structure allows for the effective conjugation with other ligands, enabling targeted protein degradation, making it an essential tool in chemical biology and therapeutic research.
Thalidomide-O-C8-Boc is a derivative of Thalidomide that functions as a ligand for the E3 ubiquitin ligase Cereblon (CRBN). This compound is utilized in the development of PROTACs by facilitating the recruitment of CRBN to target proteins through a linker. Its key biological activity involves modulating protein degradation pathways, making it valuable in drug discovery and therapeutic research targeting diseases linked to aberrant protein expressions.
Thalidomide-5-O-C4-NH2 hydrochloride is a potent ligand targeting the E3 ubiquitin ligase cereblon (CRBN). This compound facilitates the recruitment of CRBN, enabling the selective degradation of target proteins through the PROTAC (proteolysis-targeting chimera) mechanism. Thalidomide-5-O-C4-NH2 hydrochloride is instrumental in research applications focused on targeted protein degradation and the modulation of cellular pathways.
