2. Signaling Pathways
  3. PROTAC
  4. Ligands for E3 Ligase

Ligands for E3 Ligase

E3 ligase-recruiting Moiety

Ligands for E3 Ligase

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A PROTAC (Proteolysis Targeting Chimeric Molecule) is a protein degrader comprised of a ligand for E3 ligase (E3 ligase binder), a linker and a ligand for target protein (target binder). The association between an E3 ligase and a target protein induced by a PROTAC will lead to the transfer of ubiquitin and degradation of the targeted protein.

E3 ligases catalyze the transfer of ubiquitin to targeted proteins and determine the specificity of the proteins. There are hundreds of E3 ligases in cells, but only a limited number of them are successfully used in reported PROTACs, such as VHL (von Hippel-Lindau disease tumor suppressor protein), CRBN (Cereblon), MDM2 (the mouse double minute 2 homologue) and IAP (inhibitor of apoptosis).

Ligands for E3 Ligase Isoform Specific Products:

Ligands for E3 Ligase Isoform Comparison
Cat. No. Product Name CAS No. Purity Chemical Structure
  • 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-103597
    Thalidomide-O-COOH 1061605-21-7 99.85%
    Thalidomide-O-COOH (Cereblon ligand 3) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-O-COOH (Cereblon ligand 3) can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-O-COOH
  • 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-23095
    Thalidomide-5-OH 64567-60-8 99.65%
    Thalidomide-5-OH is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-OH can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-OH
  • HY-W087383
    Thalidomide 5-fluoride 835616-61-0 99.96%
    Thalidomide 5-fluoride is a thalidomide-based Cereblon ligand used to recruit Cereblon protein. Thalidomide 5-fluoride can be linked to target protein ligands (e.g. IRAK4) through a linker to form PROTAC molecules (e.g. PROTAC IRAK4 degrader-1). PROTAC IRAK4 degrader-1 caused <20%, >20-50%, and >50% IRAK4 protein degradation in OCI-LY-10 cells at concentrations of 0.01, 0.1, and 1 μM, respectively.
    Thalidomide 5-fluoride
  • HY-131717
    Thalidomide-NH-CH2-COOH 927670-97-1 98.07%
    Thalidomide-NH-CH2-COOH is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-NH-CH2-COOH can be connected to the ligand for protein by a linker to form PROTACs, such as THAL-SNS-032 (HY-123937).
    Thalidomide-NH-CH2-COOH
  • HY-103596
    Thalidomide-4-OH 5054-59-1 99.85%
    Thalidomide-4-OH (Cereblon ligand 2) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-4-OH (Cereblon ligand 2) can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-4-OH
  • HY-117937
    BC-1215 1507370-20-8 99.94%
    BC-1215 is a F-box protein 3 (Fbxo3) inhibitor. BC-1215 works by antagonizing of Fbxo3 on TRAF cytokine signaling and exhibits a low IC50 in vitro. BC-1215 can be used for the research of inflammation.
    BC-1215
  • HY-43722
    Lenalidomide-Br 2093387-36-9 99.86%
    Lenalidomide-Br (Compound 41) is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein. Lenalidomide-Br can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC STAT3 degrader SD-36 (HY-129602).
    Lenalidomide-Br
  • 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-W181530
    NCT02 790245-61-3 98.14%
    NCT02 is a molecular glue degrader based on the E3 ubiquitin ligase DDB1 that targets CDK12 and its binding partner CCNK. NCT02 triggers the ubiquitination and proteasomal degradation of CCNK, thereby downregulating CDK12 protein levels and inhibiting its downstream signaling pathways. NCT02 can induce tumor cell apoptosis, arrest the cell cycle, and selectively inhibit the proliferation of colorectal cancer cells carrying TP53 defects or belonging to the consensus molecular subtype CMS4. NCT02 has the potential to inhibit tumor growth in in vitro and in vivo models.
    NCT02
  • HY-152231
    BODIPY FL thalidomide 2740620-18-0 99.18%
    BODIPY FL thalidomide is a high-affinity fluorescent probe for human cereblon protein with a Kd value of 3.6 nM.
    BODIPY FL thalidomide
  • HY-156106
    VHL-IN-1 3033117-53-9 99.84%
    VHL-IN-1 (compound 30) is a ubiquitin E3 ligase von Hippel-Lindau (VHL) inhibitor (dissociation constant Kd=37 nM) that stabilizes and induces HIF-1α transcriptional activity. VHL-IN-1 has potential as a HIF-1α stabilizer and degrader of proteolytically targeted chimeras (PROTACs).
    VHL-IN-1
  • HY-W440247
    CRBN ligand-109 2758533-77-4 99.11%
    CRBN ligand-109 is a CRBN-type E3 ubiquitin ligase ligand that can be used to prepare PROTAC.
    CRBN ligand-109
  • HY-159646
    BMS-986397 2564486-44-6 99.76%
    BMS-986397 is a cereblon-based CK1α (casein kinase 1α) molecular glue degrader that can cause rapid apoptosis and cell cycle arrest in TP53 wild-type AML (acute myeloid leukemia) cells. BMS-986397 can be used for the study of AML and HR-MDS (High-Risk Myelodysplastic Syndrome).
    BMS-986397
  • HY-47070
    VH 101, acid 2408341-97-7 98.82%
    VH 101, acid is a functionalized von-Hippel-Lindau (VHL) protein ligand for PROTAC research and development. VH 101, acid contains an E3 ligase ligand plus an alkyl linker with terminal amine ready for conjugation to a target protein ligand.
    VH 101, acid
  • HY-125905
    VH032-cyclopropane-F 2306193-99-5 99.92%
    VH032-cyclopropane-F is the VH032-based VHL ligand. VH032-cyclopropane-F can be connected to the ligand for protein (e.g., SMARCA BD ligand) by a linker to form PROTACs (e.g., PROTAC 1). PROTAC 1 is a partial degrader of SMARCA2 and SMARCA4.
    VH032-cyclopropane-F
  • HY-125845A
    (S,S,S)-AHPC hydrochloride 2115897-23-7 99.16%
    (S,S,S)-AHPC hydrochloride is a von Hippel-Lindau (VHL) amino building block. (S,S,S)-AHPC (Compound 27) is a ligand used as a negative control for (S,R,S)-AHPC. (S,R,S)-AHPC is the VH032-based VHL ligand used in the recruitment of the VHL protein.
    (S,S,S)-AHPC hydrochloride
  • HY-153698
    CC-3060 444288-86-2 99.7%
    CC-3060 is a Cereblon modulator that promotes ZBTB16 degradation. CC-3060 degrades ZBTB16 with a DC50 of 0.47 nM in HT-1080 cells. CC-3060 targets ZBTB16 for degradation by primarily engaging distinct structural degrons on different zinc finger domains.
    CC-3060
  • HY-125292
    NV03 2448341-58-8 99.77%
    NV03 is a potent and selective antagonist of Ubiquitin-like with PHD and RING finger domains 1 (UHRF1)-H3K9me3 interaction by binding to UHRF1 tandem tudor domain, with a Kd of 2.4 μM. NV03 is also a ligand for E3 ligase. NV03 can be studied in anticancer research.
    NV03
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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