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E3 ligase ligand-linker conjugates combine a ligase ligand and a linker in one ready-to-couple PROTAC building block. Attaching such a conjugate to a target-protein ligand completes a proteolysis-targeting chimera (PROTAC) in a final coupling step. Many conjugates in this category carry a cereblon ligand derived from pomalidomide, lenalidomide or thalidomide, for example Pomalidomide-PEG4-C2-NH2 and Lenalidomide-C5-NH2. Others are built on von Hippel-Lindau (VHL) ligands, such as (S,R,S)-AHPC-C3-NH2 and VH032-thiol-C6-NH2. Terminal amines, acids and azides allow attachment by amide coupling or click chemistry.
Synonyms: Cereblon Ligand-Linker Conjugates 19; E3 ligase Ligand-Linker Conjugates 31
Lenalidomide-C5-NH2 is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C5-NH2 can be connected to the ligand for protein by a linker to form PROTACs.
VH 032 amide-alkylC5-azide is a functionalized ligand targeting the von-Hippel-Lindau (VHL) protein, specifically designed for PROTAC research and development. This compound features an E3 ligase ligand along with an alkyl linker, culminating in a terminal azide group suitable for conjugation to target protein ligands. Its unique structure facilitates the creation of innovative protein degradation systems, making it a valuable tool in chemical biology and therapeutic research.
VH032-C7-COOH is a functionalized ligand targeting the von-Hippel-Lindau (VHL) protein, primarily utilized in PROTAC (Proteolysis Targeting Chimera) research and development. This compound features an E3 ligase ligand along with an alkyl linker terminating in an amine group, facilitating the conjugation of target protein ligands. VH032-C7-COOH supports studies in targeted protein degradation, making it a valuable tool for advancing therapeutic strategies in cancer and other diseases.
(S,R,S)-AHPC-Me-C7 ester is an E3 ligase ligand-linker conjugate designed for the synthesis of BCL-XL PROTAC degraders. This compound facilitates targeted protein degradation by linking E3 ligases with substrates, thereby enabling the selective degradation of BCL-XL. It is particularly useful in studies focused on cancer therapeutics and biochemical pathways involving protein regulation.
Lenalidomide-C5-amido-Boc is a Cereblon ligand designed for the recruitment of the CRBN protein, targeting E3 ligase-mediated protein degradation pathways. This compound can be conjugated to various ligands via a spacer to produce PROTACs (proteolysis targeting chimeras), facilitating the selective degradation of specific proteins. Its application in research includes studying targeted protein elimination and elucidating protein function in various biological contexts.
Pomalidomide-PEG5-C2-NH2 hydrochloride is a Pomalidomide derivative functioning as a ligand for cereblon (CRBN), facilitating the recruitment of the CRBN protein. This compound is instrumental in the design of proteolysis-targeting chimeras (PROTACs) through its conjugation with other proteins via a linker. Its applications extend to targeted protein degradation studies and the exploration of CRBN-mediated pathways in cellular models.
Synonyms: Pomalidomide 4'-alkylC7-amine hydrochloride
Pomalidomide-C7-NH2 hydrochloride is an E3 ligase ligand-linker conjugate that aids in the development of targeted protein degraders. This compound facilitates the synthesis of PROTACs (Proteolysis Targeting Chimeras), enabling selective degradation of specific proteins within cellular systems. Its unique structure supports targeted intracellular delivery and engagement with E3 ubiquitin ligases, making it a valuable reagent for research focused on protein modulation and therapeutic applications.
Synonyms: VH032-C6-NH2 dihydrochloride
(S,R,S)-AHPC-C6-NH2 dihydrochloride is an E3 ligase ligand-linker conjugate that combines the VHL ligand derived from VH032 with a C6 linker, specifically designed for the development of AKT PROTAC degraders. This compound facilitates targeted protein degradation by recruiting E3 ligases, thereby offering significant utility in studies of protein turnover and cellular signaling pathways. It serves as a valuable tool for researchers investigating the effects of synthetic PROTACs in therapeutic contexts.
Pomalidomide-amino-PEG5-NH2 is a conjugate designed for E3 ligase modulation, utilizing a Pomalidomide-derived ligand targeting cereblon. This compound features a PEG5 linker, facilitating its application in PROTAC technology. It is valuable for studies in targeted protein degradation and related therapeutic strategies.
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LCL-PEG3-N3 is a decoy oligonucleotide ligand targeting E3 ligases, facilitating the development of chimeric molecules such as LCL-ER(dec) for the degradation of estrogen receptors. As a versatile click chemistry reagent, it features an azide functional group, enabling copper-catalyzed azide-alkyne cycloaddition (CuAAc) with alkyne-containing molecules. Additionally, LCL-PEG3-N3 can participate in strain-promoted alkyne-azide cycloaddition (SPAAC) reactions when combined with DBCO or BCN-modified entities. This compound is valuable in chemical biology applications and protein degradation studies.
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Pomalidomide-C11-NH2 hydrochloride is a potent ligand targeting the E3 ubiquitin ligase cereblon (CRBN). This compound facilitates the recruitment of CRBN, enabling the development of proteolysis-targeting chimeras (PROTACs) for targeted protein degradation. Its utility in drug discovery and molecular biology research makes it a valuable tool for studying protein regulation and associated pathways.
AHPC-PEG6-CH2COOH is a conjugate designed to facilitate interactions with E3 ligases, featuring a von Hippel-Lindau (VHL) ligand linked through a 6-unit polyethylene glycol (PEG) chain. This reagent serves as a valuable tool in the synthesis of PROTAC CMP98, enabling targeted protein degradation applications in chemical biology research. Its unique structure allows for improved solubility and bioavailability, making it suitable for various studies involving targeted protein modulation.
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(S,R,S)-AHPC-CO-PEG3-NHBoc is an E3 ligase ligand-linker conjugate designed for the synthesis of PROTAC G9a/GLP degrader 1. This compound facilitates targeted protein degradation through the selective degradation of G9a and GLP, demonstrating significant anti-cancer activity. Its application is pivotal in advancing research in protein modulation and therapeutic development in oncology.
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E3 Ligase Ligand-linker Conjugate 133 is a synthesized conjugate comprising an E3 ligase ligand and a linker, functioning as a crucial intermediate in the development of the PROTAC molecule pan-KRAS degrader 4. This compound facilitates targeted protein degradation by leveraging the ubiquitin-proteasome system, making it essential for studies related to targeted cancer therapeutics and protein modulation. Its application in PROTAC research highlights its potential in advancing therapeutic strategies against malignancies associated with KRAS mutations.
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Pomalidomide-C9-Br is an E3 ligase ligand-linker conjugate designed for the synthesis of PROTAC EGFR degrader 15, a targeted protein degradation agent. This compound exhibits significant anti-cancer activity by promoting the degradation of epidermal growth factor receptor (EGFR) through the proteasome pathway. The use of Pomalidomide-C9-Br in research applications may accelerate the development of novel therapeutics aimed at treating EGFR-driven malignancies.
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Pomalidomide-5-C7-NH2 hydrochloride is a synthetic ligand targeting the E3 ligase cereblon (CRBN). This compound facilitates the recruitment of CRBN, enabling the innovative design of PROTACs (Proteolysis Targeting Chimeras) for targeted protein degradation studies. Its unique chemical structure supports the exploration of CRBN's role in various cellular processes and therapeutic applications, such as oncology and autoimmune diseases.
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Lenalidomide 4'-alkyl-C5-azide is a functionalized cerebellar ligand designed for the development of PROTACs. This compound features an E3 ligase ligand and a long-chain alkyl group with terminal azides, facilitating the conjugation with target protein ligands. It serves as an important tool for researchers investigating targeted protein degradation and related pathways in cellular models.
(S,R,S)-AHPC-O-PEG1-propargyl is an E3 ligand utilized for the synthesis of proteolysis-targeting chimeras (PROTACs). This compound features an alkyne group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAC) reactions with azide-containing molecules. Its primary applications include facilitating targeted protein degradation studies and drug discovery efforts in chemical biology.
Thalidomide-5-F-6-azetidin-MeOH is an E3 ligase ligand-linker conjugate, specifically designed for the synthesis of PROTAC FLT3/CHK1 Degrader-1. This compound effectively targets and degrades FLT3 and CHK1, demonstrating significant anti-tumor activity. It serves as a valuable tool in drug development research, facilitating insights into targeted protein degradation mechanisms in cancer therapy.
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Synonyms: (S,R,S)-AHPC-CO-C6-COOH
VH 032 amide-alkylC6-acid is a ligand specifically targeting the von Hippel-Lindau (VHL) protein. As an analog of VH032, it plays a pivotal role in recruiting VHL for various biological processes. This compound is instrumental in the synthesis of PROTACs, facilitating targeted protein degradation for research applications in cancer biology and cellular regulation.
Pomalidomide-5-C9-NH2 hydrochloride is a potent ligand targeting the E3 ligase cereblon (CRBN). This compound facilitates the recruitment of CRBN protein, enabling targeted protein degradation. It serves as a valuable tool in the development of PROTACs (proteolysis-targeting chimeras) by linking with other ligands, thereby advancing research in cellular regulation and cancer therapeutics.
LCL-PEG3-N3 hydrochloride is a decoy oligonucleotide ligand targeting E3 ligases, facilitating the development of chimeric molecules such as LCL-ER(dec) for the degradation of estrogen receptors. This compound features an azide functional group, allowing it to participate in copper-catalyzed azide-alkyne cycloaddition reactions (CuAAc) with alkyne-bearing molecules. Additionally, it can engage in strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with reagents containing DBCO or BCN groups, making it a versatile tool for click chemistry applications in chemical biology research.
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Pomalidomide-5-C10-NH2 hydrochloride is a derivative of Pomalidomide that functions as a ligand for the E3 ubiquitin ligase cereblon (CRBN). This compound facilitates the targeted recruitment of CRBN, enabling the formation of PROTAC (proteolysis-targeting chimeras) when linked to a specific protein ligand. Pomalidomide-5-C10-NH2 hydrochloride is suitable for research applications focused on protein degradation pathways and targeted protein modulation.
A 410099.1 amide-PEG2-amine-Boc is a functionalized ligand designed for E3 ligase targeting, specifically utilized in PROTAC (Proteolysis Targeting Chimeras) applications. This compound features an IAP ligand combined with a PEG2 linker and a terminal amine, enabling efficient conjugation with target protein ligands. Its design facilitates targeted protein degradation, making it a valuable tool for studying protein function and developing novel therapeutic strategies.
Thalidomide-NH-amido-C4-Br is a versatile E3 ligase ligand-linker conjugate designed for the synthesis of protein-targeting chimeras, specifically PROTAC degraders such as BSJ-02-162. This compound facilitates targeted protein degradation through the engagement of E3 ligases, thereby modulating protein levels in various biological contexts. It is an essential tool for researchers developing innovative therapies that leverage targeted ubiquitination and degradation pathways.
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