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]

Cereblon Verwandte Produkte (429):

By Type:	Pan (10) Selective (169)

Art. -Nr.	Produktname	CAS. Nr.	Reinheit	Chemische Struktur

HY-138853A

Thalidomide-NH-amido-C8-NH2 hydrochloride	2983057-94-7
Thalidomide-NH-amido-C8-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.

HY-156162

Thalidomide-NH-C14-NH2 hydrochloride
Thalidomide-NH-C14-NH2 hydrochloride is a Thalidomide (HY-14658)-based cereblon ligand that recruits CRBN proteins. Thalidomide-NH-C14-NH2 hydrochloride can be connected to the target protein ligand through a linker to form a PROTAC molecule. For example, THAL-SNS-032 (HY-123937).

HY-161187

Thalidomide-piperidine-1,6-diazaspiro[3.3]heptane-boc
Thalidomide-piperidine-1,6-diazaspiro[3.3]heptane-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-piperidine-1,6-diazaspiro[3.3]heptane-boc can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.

HY-138855

Thalidomide-NH-amido-PEG2-C2-NH2	2983036-90-2
Thalidomide-NH-amido-PEG2-C2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.

HY-161189

Thalidomide-2,6-diazaspiro[3.4]octane-C-piperidine-C2-O-C-boc
Thalidomide-2,6-diazaspiro[3.4]octane-C-piperidine-C2-O-C-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-2,6-diazaspiro[3.4]octane-C-piperidine-C2-O-C-boc can serve as Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.

HY-134985

Thalidomide-NH-PEG1-NH2	2138439-12-8
Thalidomide-NH-PEG1-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.

HY-138860

Thalidomide-O-C11-acid	3023879-35-5
Thalidomide-O-C11-acid is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.

HY-157749

Thalidomide-piperazine-(S)-CH2-pyrrolidine-C2-O-CH2-COO-C(CH3)3
Thalidomide-piperazine-(S)-CH2-Pyrrolidine-C2-O-CH2-COO-C (CH3)3 is a synthetic E3 ligase ligand-Linker conjugate. Thalidomide-piperazine-(S)-Ch2-Pyrrolidine-C2-O-CH2-COO-C(CH3)3 includes Thalidomide-based cereblon ligands and linkers. Thalidomide-piperazine-(S)-CH2-Pyrrolidine-C2-O-CH2-COO-C(CH3)3 can be used to synthesize PROTAC BET.

HY-141014

Thalidomide-O-PEG4-Boc	2411681-87-1
Thalidomide-O-PEG4-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.

HY-138851A

Thalidomide-NH-amido-C5-NH2 hydrochloride
Thalidomide-NH-amido-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.

HY-W998329

Thalidomide-O-amide-C5-NH2 hydrochloride	2716130-28-6
Thalidomide-O-amide-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.

HY-161195

Deoxy-thalidomide-piperidine-C-piperazine-C-boc
Deoxy-thalidomide-piperidine-C-piperazine-C-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Deoxy-thalidomide-piperidine-C-piperazine-C-boc can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.

HY-W584517

Thalidomide-5-O-CH2-COO(t-Bu)	2682112-10-1
Thalidomide-5-O-CH2-COO(t-Bu) is a t-Bu modified Thalidomide (HY-14658), which acts as a Cereblon ligand to recruit CRBN protein. The t-Bu protecting group at the end of Thalidomide-5-O-CH2-COO(t-Bu) can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-5-O-CH2-COO(t-Bu) is a key intermediate in the synthesis of CRBN-based PROTAC molecules.

HY-138857

Thalidomide-NH-amido-PEG4-C2-NH2	2653336-34-4
Thalidomide-NH-amido-PEG4-C2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.

HY-159165

Pomalidomide-cyclopentane-amide-Alkyne
Pomalidomide-cyclopentane-amide-Alkyne is an E3 ligase ligand-linker conjugate that incorporates the Pomalidomide (HY-10984) and the linker cyclopentane-amide-Alkyne. Pomalidomide-cyclopentane-amide-Alkyne is used to form PROTACs, such as RGB110 (HY-159087).

HY-156165

Thalidomide-5-NH-PEG3-NH2 hydrochloride	2863635-01-0
Thalidomide-5-NH-PEG3-NH2 hydrochloride is a Thalidomide (HY-14658)-based cereblon ligand that recruits CRBN proteins. Thalidomide-5-NH-PEG3-NH2 hydrochloride can be connected to the target protein ligand through a linker to form a PROTAC molecule. For example, THAL-SNS-032 (HY-123937).

HY-138849

Thalidomide-NH-amido-C2-NH2	2763827-10-5
Thalidomide-NH-amido-C2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.

HY-168389

Thalidomide-piperidine-C2-piperazine-Boc
Thalidomide-piperidine-C2-piperazine-Boc is an E3 ligase ligand-linker conjugate that incorporates the Thalidomide (HY-130639) based cereblon ligand and a linker used in PROTAC technology. Thalidomide-piperidine-C2-piperazine-Boc can be used for synthesis of PROTACs.

HY-139544

Thalidomide-5-propoxyethanamine	2357107-60-7
Thalidomide-5-propoxyethanamine is the Thalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein.

HY-172145

Thalidomide-O-CH2-CO-NH-C2-PEG2-NH-Boc	1957235-73-2
Thalidomide-O-COOH-NH2-C2-PEG2-NH-Boc is a conjugate of E3 ligase ligand and linker, which contains Thalidomide-based CEREBLON ligand and PEG inker. Thalidomide-O-COOH-NH2-C2-PEG2-NH-Boc can be used to synthesize PROTAC degrader JB300 (HY-137341).

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