Cereblon
Cereblon (CRBN) functions as the substrate receptor of the CRL4 E3 ubiquitin ligase, mediating protein ubiquitination and degradation[1]. Mechanistically, CRBN regulates the Wnt signaling pathway by targeting Casein kinase 1α (CK1α), a negative regulator of β-Catenin, for degradation[1]. This Wnt-dependent modulation of CRBN influences developmental and disease-relevant phenotypes in zebrafish and Drosophila models[1]. Clinically, CRBN mutations have been identified in multiple myeloma patients with extramedullary disease, conferring resistance to immunomodulatory drugs (IMiDs) and highlighting its role in drug responsiveness[2]. Notably, these mutations include a Q99 truncating mutation and an R283K point mutation, impairing CRBN-mediated anti-myeloma activity[2]. Compared with related ubiquitin ligase substrate receptors, CRBN exhibits unique specificity for neo-substrates under both IMiD-bound and unbound conditions, distinguishing its functional isoform-dependent effects[1][2]. CRBN-targeted agonists, including IMiDs, exploit this substrate specificity to induce selective protein degradation, providing a basis for experimental modulation of Wnt and cancer-related pathways[1][2]. Therefore, CRBN serves as a central regulator of ubiquitin-mediated proteostasis, bridging signal transduction, disease pathophysiology, and therapeutic interventions[1][2].
References:
- [1]. Shen C, et al. The E3 ubiquitin ligase component, Cereblon, is an evolutionarily conserved regulator of Wnt signaling. Nat Commun. 2021 Sep 6;12(1):5263. [Content Brief]
- [2]. Egan JB, et al. Extramedullary myeloma whole genome sequencing reveals novel mutations in Cereblon, proteasome subunit G2 and the glucocorticoid receptor in multi drug resistant disease. Br J Haematol. 2013 Jun;161(5):748-751. [Content Brief]
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Cereblon Related Products (437)
Related Products (437)
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Pomalidomide-PEG4-C2-NH2 hydrochloride
0 ImagesPomalidomide-PEG4-C2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 4-unit PEG linker used in the synthesis of PROTACs..
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Pomalidomide-PEG3-azide
0 ImagesPomalidomide-PEG3-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology. Pomalidomide-PEG3-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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Pomalidomide-PEG4-C-COOH
0 ImagesSynonyms: Cereblon Ligand -Linker Conjugates 1; E3 Ligase Ligand-Linker Conjugates 1Pomalidomide-PEG4-C-COOH (Cereblon Ligand -Linker Conjugate 1) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 4-unit PEG linker used in PROTAC technology.
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Pomalidomide-PEG1-C2-N3
0 ImagesSynonyms: Cereblon Ligand-Linker Conjugates 13; E3 ligase Ligand-Linker Conjugates 50
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Pomalidomide-C3-NHS ester
0 ImagesPomalidomide-C3-NHS ester is a synthesized E3 ligase ligand-linker conjugate, incorporating the Pomalidomide based cereblon ligand and NHS ester linker.
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Lenalidomide 4'-PEG3-amine dihydrochloride
0 ImagesLenalidomide 4'-PEG3-amine dihydrochloride is a lenalidomide (HY-A0003)-derived immunomodulator and monofunctional synthetic intermediate, as well as a E3 ubiquitin ligase ligand. Lenalidomide 4'-PEG3-amine dihydrochloride can be used for the preparation of small-molecule drug conjugates and heterobifunctional protein degraders.
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Pomalidomide-PEG4-azide
0 ImagesPomalidomide-PEG4-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology. Pomalidomide-PEG4-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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Thalidomide-PEG2-C2-NH2 hydrochloride
0 ImagesSynonyms: Thalidomide-NH-PEG2-C2-NH2 hydrochlorideThalidomide-PEG2-C2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 2-unit PEG linker used in PROTAC technology.
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Thalidomide-O-amido-PEG4-azide
0 ImagesThalidomide-O-amido-PEG4-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Thalidomide-O-amido-PEG4-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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Pomalidomide 4'-PEG3-azide
0 ImagesCat. No.: HY-130652CAS No.: 2271036-46-3Pomalidomide 4'-PEG3-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide-based cereblon ligand and a linker. Pomalidomide 4'-PEG3-azide can be used for the synthesis of iRucaparib-TP3 (Compound 3). iRucaparib-TP3 is a highly efficient PARP1?degrader based on Rucaparib by using the PROTAC approach. Pomalidomide 4'-PEG3-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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Thalidomide-propargyl
0 ImagesThalidomide-propargyl is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-propargyl can be connected to the ligand for protein by a linker to form the IMiD containing PROTACs. Thalidomide-propargyl is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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Lenalidomide-C4-NH2 hydrochloride
0 ImagesCat. No.: HY-115446ACAS No.: 2435715-90-3Synonyms: Cereblon ligand 1 hydrochloride; E3 ligase Ligand-Linker Conjugates 32 hydrochlorideLenalidomide-C4-NH2 hydrochloride is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C4-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTAC (Compound 24), which has IC50s of 0.98 nM and 13.7 nM in inhibition of RS4;11 and MOLM-13 acute leukemia cell lines growth, respectively.
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Thalidomide-NH-PEG3-propionic acid
0 ImagesThalidomide-NH-PEG3-propionic acid is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.
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Thalidomide-NH-C5-NH2 hydrochloride
0 ImagesThalidomide-NH-C5-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
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Pomalidomide-C2-NH2 hydrochloride
0 ImagesSynonyms: Cereblon Ligand-Linker Conjugates 15 hydrochloridePomalidomide-C2-NH2 (Cereblon Ligand-Linker Conjugate 15) hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology.
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Thalidomide-Piperazine 5-fluoride
0 ImagesCat. No.: HY-134983CAS No.: 2222114-22-7Thalidomide-piperazine hydrochloride is a synthetic E3 ligase ligand-linker conjugate, containing a cereblon ligand based on Thalidomide (HY-14658) and one linker. Thalidomide-piperazine hydrochloride can be used in studies related to PROTAC synthesis.
