2. Signaling Pathways
  3. PROTAC
  4. Ligands for E3 Ligase
  5. Cereblon Isoform

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].

Cereblon 관련 제품 (911):

Cat. No. 상품명 CAS No. Purity 화학구조
  • HY-10984
    Pomalidomide 19171-19-8 99.96%
    Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.
    Pomalidomide
  • HY-A0003
    Lenalidomide 191732-72-6 99.94%
    Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells.
    Lenalidomide
  • HY-101488
    CC-885 1010100-07-8 99.26%
    CC-885 is a cereblon (CRBN) modulator with potent anti-tumour activity. CC-885 is also a known degrader of GSPT1, inhibiting protein translation.
    CC-885
  • HY-101291
    Iberdomide 1323403-33-3 99.54%
    Iberdomide (CC-220) is an orally active and potent cereblon (CRBN) E3 ligase modulator (CELMoD) with an IC50 of ~150 nM for cereblon-binding affinity. Iberdomide, a derivative of Thalidomide (HY-14658), has antitumor and immunostimulatory activities.
    Iberdomide
  • HY-130800
    Eragidomide 1860875-51-9 99.93%
    Eragidomide (CC-90009) is a first-in-class GSPT1-selective cereblon (CRBN) E3 ligase modulator, acts as a molecular glue. Eragidomide coopts the CRL4CRBN to selectively target GSPT1 for ubiquitination and proteasomal degradation.
    Eragidomide
  • HY-W593794
    E3 ligase Ligand 79 2152672-96-1 99.07%
    E3 ligase Ligand 79 is a CRBN E3 ligase ligand that can be used for synthesis of PROTACs.
    E3 ligase Ligand 79
  • HY-W1005059
    N-Methylthalidomide 42472-93-5
    N-Methylthalidomide is a cereblon ligand derivative that acts as an E3 ubiquitin ligase ligand for the synthesis of PROTAC LLC0424N (HY-185557). LLC0424N serves as a negative control for NSD2 PROTAC degrader LLC0424 (HY-161574), with weak ability to induce NSD2 degradation and low growth inhibitory effect on cancer cells carrying NSD2 mutations.
    N-Methylthalidomide
  • HY-D3392
    Thalidomide-cyanine 5
    Thalidomide-cyanine 5 is a fluorescent probe prepared by conjugating the CRBN binder Thalidomide (HY-14658) with the near-infrared fluorescent dye Cy5. Thalidomide-cyanine 5 binds to DDB1-CRBN protein complex with a Kd of 121.6 nM. Thalidomide-cyanine 5 binds to CRBN to form a binary complex, and is mainly used for the visual tracking research of degradants such as PROTAC (Ex/Em = 650/665 nm).
    Thalidomide-cyanine 5
  • HY-160695
    PT-179 2924858-25-1 99.91%
    PT-179 is an orthogonal Thalidomide (HY-14658) derivative that targets cereblon without causing off-target degradation effects. PT-179 is able to specifically bind CRBN, form a ternary complex with a target protein fused to a zinc finger (ZF) degron, and mediate the degradation of the tagged protein. For example, PT-179 binds to the ubiquitin ligase substrate receptor cereblon by forming a complex with SD40 and efficiently degrades proteins N- or C-terminally fused to SD40 or SD36 (DC50 for eGFP: 4.5 nM and 14.3 nM). PT-179 can be used to develop compact protein degradation tagging platforms.
    PT-179
  • HY-146237
    Golcadomide 2379572-34-4 98.04%
    Golcadomide (CC-99282) is a potent and orally active CRBN E3 ligase modulator (CELMoD). Golcadomide interacts with the CRL4 CRBN E3 ubiquitin ligase substrate receptor CRBN, inducing the recruitment and ubiquitin-mediated proteasomal degradation of the transcription factors Ikaros and Aiolos. Golcadomide shows potential for research in cancer-related fields, including chronic lymphocytic leukemia (CLL) and non-Hodgkin lymphoma (NHL).
    Golcadomide
  • HY-159646
    BMS-986397 2564486-44-6 99.76%
    BMS-986397 is a potent, selective, and orally active cereblon-based molecular glue degrader of casein kinase 1α (CK1α). BMS-986397 induces apoptosis and cell cycle arrest in acute myeloid leukemia (AML) cells. BMS-986397 is a promising agent for the investigation of AML and high-risk myelodysplastic syndromes (HR-MDS).
    BMS-986397
  • HY-A0003B
    Lenalidomide hemihydrate 847871-99-2 99.98%
    Lenalidomide hemihydrate (CC-5013 hemihydrate), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hemihydrate is an orally active immunomodulator. Lenalidomide hemihydrate (CC-5013 hemihydrate) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide hemihydrate (CC-5013 hemihydrate) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells.
    Lenalidomide hemihydrate
  • HY-45512
    E3 ligase Ligand 63 2304754-51-4 99.80%
    E3 ligase Ligand 63 is an E3 ligase ligand that can be used to synthesize CDK2 degrader 2 (HY-163815).
    E3 ligase Ligand 63
  • HY-W593975
    CRBN ligand-547 2446913-88-6 99.82%
    CRBN ligand-547 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. CRBN ligand-547 can be linked to a target protein ligand via a linker to form a PROTAC.
    CRBN ligand-547
  • HY-153698
    CC-3060 444288-86-2 99.7%
    CC-3060 is a molecular glue modulator targeting Cereblon (CRBN) E3 ubiquitin ligase and ZBTB16 degrader with a DC50 of 0.47 nM in HT-1080 cells. CC-3060 engages structural degrons on ZBTB16’s ZnF1 or ZnF3 domains for fusion protein substrates. CC-3060 can be used for the research of acute promyelocytic leukemia.
    CC-3060
  • HY-137206
    ALV2 2438124-95-7 98.05%
    ALV2 is a potent and selective Helios molecular glue degrader. ALV2 binds CRBN, with an IC50 of 0.57 μM. Helios is the zinc-finger transcription factor that can maintain a stable Treg cell phenotype in the inflammatory tumor microenvironment.
    ALV2
  • HY-145776
    ALV1 2438124-79-7 98.62%
    ALV1 is a molecular glue degrader for Ikaros (IKZF1) and Helios (IKZF2) with DC50 of 2.5 nM and 10.3 nM respectively. ALV1 bind CRBN with an IC50 of 0.55 μM, and induces CRBN-Helios dimerization. ALV1 can be used to study the properties and functions of regulatory T cells.
    ALV1
  • HY-W440247
    CRBN ligand-109 2758533-77-4 99.62%
    CRBN ligand-109 is a CRBN-type E3 ubiquitin ligase ligand that can be used to prepare PROTAC.
    CRBN ligand-109
  • HY-152231
    BODIPY FL thalidomide 2740620-18-0 99.18%
    BODIPY FL thalidomide is a high-affinity and selective human cereblon (CRBN)-targeting fluorescent probe with a Kd of 3.6 nM. BODIPY FL thalidomide enables use as a probe in time-resolved fluorescence resonance energy transfer (TR-FRET) binding assays for cereblon ligands. BODIPY FL thalidomide supports development of highly sensitive, selective, stable cereblon TR-FRET binding assays (Ex/Em = 502/510 nm).
    BODIPY FL thalidomide
  • HY-W442918
    CRBN ligand-881 92137-90-1 99.30%
    CRBN ligand-881 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. CRBN ligand-881 can be linked to a target protein ligand via a linker to form a PROTAC.
    CRBN ligand-881