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CRBN molecular glue

" in MedChemExpress (MCE) Product Catalog:

33

Inhibitors & Agonists

1

Screening Libraries

4

Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-173614

    Molecular Glues E1/E2/E3 Enzyme Cancer
    CC-647 is a molecular glue modulator targeting Cereblon (CRBN) E3 ubiquitin ligase. CC-647 promotes the interaction between CRBN and ZBTB16 as well as its oncogenic fusion protein RARα-ZBTB16 (with a DC50 of 103 nM). CC-647 is promising for research of ZBTB16-RARα-associated acute promyelocytic leukemia (APL) .
    CC-647
  • HY-173154A

    Molecular Glues NEKs Inflammation/Immunology
    NK7-902 TFA is a CRBN molecular glue degrader of NEK7. NK7-902 TFA fully degrades NEK7 in human primary monocytes and whole blood but only partially inhibits NLRP3-dependent IL-1β production. NK7-902 TFA leads to profound and long-lasting NEK7 degradation but only transiently blocks NLRP3 inflammasome activation in non-human primates by oral administration. NK7-902 TFA shows activity in murine systems .
    NK7-902 TFA
  • HY-153803

    PROTACs Molecular Glues Btk Cancer
    GBD-9 is a degrader based on the E3 ubiquitin ligase CRBN that targets BTK and the G1 to S phase transition protein GSPT1. GBD-9 has both PROTAC and molecular glue properties by inducing ubiquitination and proteasomal degradation of target proteins. GBD-9 can efficiently degrade wild-type and mutant BTK (such as C481S mutation) and GSPT1. GBD-9 significantly inhibits tumor cell proliferation by inducing G1 phase arrest in cancer cells, downregulating anti-apoptotic proteins (BCL-2, MCL-1) and activating Caspase-3 to induce apoptosis. GBD-9 is mainly used in the research of hematological tumors such as diffuse large B-cell lymphoma (DLBCL) and acute myeloid leukemia (AML) .
    GBD-9 is composed of E3 ubiquitin ligase ligand (pink part) 5-Aminothalidomide (HY-W023573), target protein ligand (blue part) Btk Inhibitor: IBT6A (HY-13036A), and PROTAC linker (black part) Nonanoic acid (HY-N7057).
    GBD-9
  • HY-164891

    Molecular Glues Others
    EM12-FS is a cereblon (CRBN) ligand that binds CRBN at His353 and a molecular glue degrader of NTAQ1. EM12-FS has a human plasma half-life of 196 min .
    EM12-FS
  • HY-130800
    Eragidomide
    4 Publications Verification

    CC-90009

    Ligands for E3 Ligase Molecular Glues Apoptosis Inflammation/Immunology Cancer
    Eragidomide (CC-90009) is a first-in-class GSPT1-selective cereblon (CRBN) E3 ligase modulator, acts as a molecular glue. Eragidomide coopts the CRL4 CRBN to selectively target GSPT1 for ubiquitination and proteasomal degradation .
    Eragidomide
  • HY-145776

    Molecular Glues Ligands for E3 Ligase IKZF Family Interleukin Related Inflammation/Immunology Cancer
    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-137206

    Molecular Glues Ligands for E3 Ligase Cancer
    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-175742

    Ligands for E3 Ligase Molecular Glues Histone Acetyltransferase Cardiovascular Disease
    BMS-986470, a HbF-activating CRBN E3 ligase modulator (CELMoD), is an orally active dual molecular glue degrader targeting ZBTB7A and WIZ. BMS-986470 has potent γ-globin induction activity. BMS-986470 can be used for sickle cell disease (SCD) research .
    BMS-986470
  • HY-176347S

    Isotope-Labeled Compounds Cancer
    Alpha Feto Protein, Arg- 13C36, 15N4, Lys- 13C6, 15N2 is the 13C- and 15N-labeled Alpha Feto Protein.
    Alpha Feto Protein, Arg-13C6,15N4, Lys-13C6,15N2
  • HY-159098

    Molecular Glues Histone Acetyltransferase Others
    dWIZ-1 is a potent WIZ molecular glue degrader. dWIZ-1 recruitments WIZ(ZF7) to cereblon (CRBN) induces WIZ degradation. dWIZ-1 has the potential for the research of sickle cell disease (SCD) .
    dWIZ-1
  • HY-172770

    Molecular Glues Cancer
    KMG-1068 (Compound 4a), a molecular glue, is a GSPT1/2 degrader. KMG-1068 effectively induces the CRBN-dependent degradation of GSPT1/2 by binding to the IMiD binding site on CRBN, facilitating the formation of a ternary complex with GSPT1/2. KMG-1068 is promising for research of cancers .
    KMG-1068
  • HY-169077

    Molecular Glues IKZF Family Cancer
    IKZF3 degrader 1 (compound 19a) is a molecular glue degrader of IKZF3 (EC50=0.012 μM). IKZF3 degrader 1 promotes the binding of IKZF3 to Cereblon (CRBN), leading to the ubiquitination and degradation of IKZF3 .
    IKZF3 degrader 1
  • HY-175453

    Molecular Glues Neurological Disease Cancer
    MRT-23227 is a molecular glue degrader that targets cereblon (CRBN). MRT-23227 forms a ternary complex with CRBN and G3BP2, activating the ubiquitin-proteasome system, leading to G3BP2 degradation. MRT-23227 has potential applications in the research of G3BP2-related cancers (such as breast and lung cancer) and neurodegenerative diseases .
    MRT-23227
  • HY-175334

    Molecular Glues Cancer
    DHC-286 is a molecular glue degrader targeting GSPT1. DHC-286 recruits GSPT1 to the CRL4CRBN ubiquitin ligase complex, promoting GSPT1 ubiquitination and proteasomal degradation, inducing cytotoxicity. DHC-286 is promising for research of cancers such as acute myeloid leukemia .
    DHC-286
  • HY-14658
    Thalidomide
    15+ Cited Publications

    Ligands for E3 Ligase Autophagy Apoptosis Molecular Glues Inflammation/Immunology Cancer
    Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ∼250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide can work as molecular glue to potentiate substrate.
    Thalidomide
  • HY-163814

    Molecular Glues CDK Cancer
    CDK2 degrader 1 (Compound 3) is a selective CDK2 molecular glue degrader with a Dmax (CDK2) of > 80% and a Ki (CRBN) > 1 μM. CDK2 degrader 1 binds to cereblon to induce ubiquitination and subsequent proteasomal degradation of the CDK2. CDK2 degrader 1 is used in the research of a wide range of cancers .
    CDK2 degrader 1
  • HY-175749

    Wee1 Cancer
    BMS-986463, a CRBN E3 ligase modulator (CELMoD), is a WEE1 kinase molecular glue degrader. BMS-986463 significantly inhibits tumor regression and reduces the level of phospho-CDK2. BMS-986463 can be used for advanced malignant solid tumors like non-small cell lung cancer (NSCLC) research .
    BMS-986463
  • HY-A0003B
    Lenalidomide hemihydrate
    Maximum Cited Publications
    50 Publications Verification

    CC-5013 hemihydrate

    Ligands for E3 Ligase Molecular Glues Apoptosis Cancer
    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-174329

    Molecular Glues Neurological Disease Cancer
    mrt-5702D is a molecular glue degrader targeting cereblon (CRBN). mrt-5702D forms a CRBN-MRT-5702D-G3BP2 ternary complex to activate the ubiquitin-proteasome system for G3BP2 degradation. mrt-5702D is promising for research of G3BP2-related cancers (e.g., breast cancer, lung cancer) and neurodegenerative diseases .
    mrt-5702D
  • HY-A0003
    Lenalidomide
    Maximum Cited Publications
    50 Publications Verification

    CC-5013

    Ligands for E3 Ligase Molecular Glues Apoptosis Inflammation/Immunology Cancer
    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-A0003A

    CC-5013 hydrochloride

    Ligands for E3 Ligase Molecular Glues Inflammation/Immunology Cancer
    Lenalidomide hydrochloride (CC-5013 hydrochloride), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hydrochloride is an orally active immunomodulator. Lenalidomide hydrochloride (CC-5013 hydrochloride) 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 hydrochloride (CC-5013 hydrochloride) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
    Lenalidomide hydrochloride
  • HY-14658R

    Ligands for E3 Ligase Autophagy Apoptosis Reference Standards Inflammation/Immunology Cancer
    Thalidomide (Standard) is the analytical standard of Thalidomide. This product is intended for research and analytical applications. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ∼250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide can work as molecular glue to potentiate substrate.
    Thalidomide (Standard)
  • HY-144998

    IKZF Family Molecular Glues Inflammation/Immunology Cancer
    NVP-DKY709 is an orally active and selective IKZF2 molecular glue degrader with the Dmax and DC50 of 53% and 4 nM, respectively. In addition, NVP-DKY709 can degrade IKZF4 (DC50: 13 nM) and SALL4 (DC50: 2 nM). NVP-DKY709 exerts anti-tumor activity by binding with CRBN to change conformation and recruit and degrade IKZF2 .
    NVP-DKY709
  • HY-A0003S

    CC-5013-d5

    Isotope-Labeled Compounds Ligands for E3 Ligase Molecular Glues Apoptosis Inflammation/Immunology Cancer
    Lenalidomide-d5 is deuterium labeled Lenalidomide. 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-d5
  • HY-A0003BR

    Ligands for E3 Ligase Molecular Glues Apoptosis Cancer
    Lenalidomide (hemihydrate) (Standard) is the analytical standard of Lenalidomide (hemihydrate). This product is intended for research and analytical applications. 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 (Standard)
  • HY-A0003R

    CC-5013 (Standard)

    Reference Standards Ligands for E3 Ligase Molecular Glues Apoptosis Inflammation/Immunology Cancer
    Lenalidomide (Standard) is the analytical standard of Lenalidomide. This product is intended for research and analytical applications. 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 (Standard)
  • HY-170820

    Molecular Glues Cancer
    XYD049 (compound 7d) is a CRBN-type molecular glue targeting GSPT1 (DC50=19 nM), which can be used for the research of MYC-driven castration-resistant prostate cancer (CRPC). XYD049 can effectively inhibit the growth of 22Rv1 cells (IC50=7 nM) and has in vivo antitumor efficacy. XYD049 downregulates the CRPC-related oncogenes in 22Rv1 cells, including AR, AR-v7, PSA, and c-Myc. XYD049 is composed of a molecular glue linker (black part) NH2-C5-NH-Boc (HY-W004710), a CRBN-type E3 ligase ligand (blue part) Thalidomide 4-fluoride (HY-41547), and a target protein ligand (red part) GSPT1 ligand-1 (HY-170821), in which the E3 ligase ligand + liner form a conjugate E3 Ligase Ligand-linker Conjugate 158 (HY-170822) .
    XYD049
  • HY-A0003S2

    CC-5013-13C5,15N

    Ligands for E3 Ligase Apoptosis Molecular Glues Isotope-Labeled Compounds Inflammation/Immunology Cancer
    Lenalidomide- 13C5, 15N is 15N and 13C labeled Lenalidomide (HY-A0003). 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-13C5,15N
  • HY-A0003S3

    CC-5013-d4

    Isotope-Labeled Compounds Apoptosis Molecular Glues Ligands for E3 Ligase Inflammation/Immunology Cancer
    Lenalidomide-d4 (CC-5013-d4) is deuterium labeled Lenalidomide. 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-d4
  • HY-176128

    PROTACs Androgen Receptor Molecular Glues Cancer
    BWA-6047 is a dual AR/AR-V7 and GSPT1 PROTAC degrader (AR: DC50 = 3.7 nM; AR-V7: DC50 = 3.0 nM; GSPT1: DC50 = 1.2 nM). BWA-6047 promotes ubiquitination and degradation of AR/AR-V7 and, through its molecular glue properties, induces the formation of a PPI between GSPT1 and CRBN, leading to GSPT1 degradation. BWA-6047 can be used in prostate cancer research (Pink: AR/AR-V7 ligand (HY-176129); Blue: E3 CRBN ligand (HY-W069604); Black: linker (HY-W069604)) .
    BWA-6047
  • HY-173154

    Molecular Glues NEKs Inflammation/Immunology
    NK7-902 is a CRBN molecular glue degrader of NEK7. NK7-902 fully degrades NEK7 in human primary monocytes and whole blood but only partially inhibits NLRP3-dependent IL-1β production. NK7-902 leads to profound and long-lasting NEK7 degradation but only transiently blocks NLRP3 inflammasome activation in non-human primates by oral administration. NK7-902 shows activity in murine systems .
    NK7-902
  • HY-174371

    Molecular Glues Casein Kinase MDM-2/p53 MALT1 Cancer
    INNO-220 is an orally active, CRBN-dependent molecular glue degrader targeting CK1α. INNO-220 induces cell cycle arrest at G0/G1 phase and triggers apoptosis by degrading CK1α. INNO-220 disrupts the assembly and function of the CARD11/BCL10/MALT1 complex, thereby inhibiting NF-κB signaling in stimulated T cells and lymphoma cells that harbor an activating mutation in CARD11. INNO-220 provides a new direction for lymphoma research.
    INNO-220
  • HY-172930

    Molecular Glues IKZF Family Potassium Channel Inflammation/Immunology Cancer
    PVTX-405 is a selective and oral active IKZF2 molecular glue degrader with a DC50  of  0.7 nM and a Dmax of 91%. PVTX-405 enhances degradation efficiency, significantly reduces off-target degradation, and alleviates hERG inhibition with IC50 of 48 µM. PVTX-405 significantly inhibits the growth of MC38 tumors, with greater synergistic anti-cancer efficacy in combination with immune checkpoint therapies (ICTs) (anti-PD1 or anti-LAG3) in the MC38 mouse tumor xenograft model using Crbn 391V C57BL/6 mice .
    PVTX-405

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