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-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-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-W012479
    H-D-Trp-OH 153-94-6 99.97%
    H-D-Trp-OH (D-Tryptophan) is the D-isomer of tryptophan, which is occasionally found in natural peptides, such as marine toxin peptides. H-D-Trp-OH can increase intestinal microbial diversity and counteract the inhibitory effect of allergic airway inflammation on intestinal microbial diversity.
    H-D-Trp-OH
  • 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
  • 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-143346
    CCW16 2361138-33-0 98.73%
    CCW16 is a cofactor for the synthesis of protein degraders, such as PROTACs CCW 28-3 (HY-156774).
    CCW16
  • HY-24538
    CRBN ligand-880 1267337-47-2 99.96%
    CRBN ligand-880 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. CRBN ligand-880 can be linked to a target protein ligand via a linker to form a PROTAC.
    CRBN ligand-880
  • 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-W072954
    Lenalidomide-5-Br 1010100-26-1 99.87%
    Lenalidomide-5-Br is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-5-Br can be connected to the ligand for protein by a linker to form PROTAC.
    Lenalidomide-5-Br
  • 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-14658A
    (S)-Thalidomide 841-67-8 99.52%
    (S)-Thalidomide ((S)-(-)-Thalidomide) is the S-enantiomer of Thalidomide. (S)-Thalidomide has immunomodulatory, anti-inflammatory, antiangiogenic and pro-apoptotic effects. (S)-Thalidomide induces teratogenic effects by binding to cereblon (CRBN) .
    (S)-Thalidomide
  • HY-W998293
    CRBN ligand-397 2736511-32-1 98.77%
    CRBN ligand-397 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. CRBN ligand-397 can be linked to a target protein ligand via a linker to form a PROTAC.
    CRBN ligand-397
  • HY-159647
    PLX-4545 2892065-45-9
    PLX-4545 is an orally active, selective molecular glue degrader targeting IKZF2. Through a molecular glue mechanism, PLX-4545 binds to CRBN, recruits IKZF2 to form a ternary complex, and promotes its ubiquitination and proteasomal degradation. This further converts inhibitory regulatory T cells (Treg) into effector-like T cells, enhances CD8+ T cell responses, and modulates the Teff:Treg balance. PLX-4545 also increases the production of the inflammatory cytokine IL-2 and reduces the suppressive activity of Treg. PLX-4545 can be used in cancer immunotherapy research, and exhibits a synergistic effect when combined with immune checkpoint inhibitors such as anti-PD1.
    PLX-4545
  • 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-130684
    MDM2 ligand 5 1410737-09-5 98.02%
    MDM2 ligand 5 is a Ligand for E3 Ligase that can be used for the synthesis of PROTACs.
    MDM2 ligand 5
  • HY-131318
    Lenalidomide-I 2207541-30-6 99.84%
    Lenalidomide-I (Compound 72), an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, is used in the recruitment of CRBN protein. Lenalidomide-I can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC BET degrader QCA570 (HY-112609).
    Lenalidomide-I
  • HY-49385
    E3 ligase Ligand 64 2760850-50-6 ≥98.0%
    E3 ligase Ligand 64 is a ligand for E3 ligase, used for the synthesis of RP03707 (HY-176134) .
    E3 ligase Ligand 64
  • HY-149934
    DCAF1 binder 1 3053860-67-3 99.12%
    DCAF1 binder 1 is a selective for the CRL4 DCAF1 E3 ligase complex. DCAF1 binder 1 is a ligands for E3 Ligase, involving in targeted protein degradation (TPD).
    DCAF1 binder 1
  • HY-125845A
    (S,S,S)-AHPC hydrochloride 2115897-23-7 99.16%
    (S,S,S)-AHPC ((S,S,S)-VH032-NH2) 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 (HY-125845). (S,R,S)-AHPC is the VH032-based VHL ligand used in the recruitment of the VHL protein.
    (S,S,S)-AHPC hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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