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

Ligands for E3 Ligase

E3 ligase-recruiting Moiety

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).

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-139548
    Thalidomide-5-methyl 40313-92-6 99.87%
    Thalidomide-5-methyl is the Thalidomide (HY-14658)-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Thalidomide-5-methyl can be used to synthesize PROTAC.
    Thalidomide-5-methyl
  • HY-W342590
    CRBN ligand-9 55003-81-1 98.0%
    CRBN ligand-9 (Compound 4d) is a CRBN ligand (Ki: 8.9 μM). CRBN ligand-9 can be used for synthesis of PROTACs.
    CRBN ligand-9
  • HY-111823
    VH032 thiol 2098836-54-3
    VH032 thiol (VHL ligand 6) is a VHL ligand, which binds to pan-BET inhibitor JQ1 via a linker to form PROTAC.
    VH032 thiol
  • HY-156499
    RNF114 ligand 1 900137-36-2
    RNF114 ligand 1 is an E3 Ubiquitin ligase RNF114 ligand.
    RNF114 ligand 1
  • HY-157512
    SJF-0661 2413035-43-3 99.2%
    SJF-0661 is a variant of the von Hippel-Lindau (VHL) protein ligand with no targeted degradation ability and can be used as a control reagent for the VHL ubiquitin ligase ligand. SJF-0661 is a variant obtained by inverting the stereocenter of the key hydroxyproline group in the VHL ligand.
    SJF-0661
  • 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-151227
    VL285 Phenol 1448188-69-9 98.56%
    VL285 Phenol is a phenol-based VL285 analog. VL285 is an E3 ubiquitin ligase VHL ligand and can be used in the synthesis of HaloPROTAC3, degrading HaloTag7 fusion protein (IC50=0.34 μM).
    VL285 Phenol
  • HY-W733888
    CRBN ligand-187 2883704-28-5
    CRBN ligand-187 is a CRBN-type E3 ubiquitin ligase ligand that can be used for synthesis of TQ-3959 (HY-175541).
    CRBN ligand-187
  • HY-10984S3
    Pomalidomide-15N,13C5
    Pomalidomide-15N,13C5 is 15N and 13C labeled Pomalidomide (HY-10984). 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-<sup>15</sup>N,<sup>13</sup>C<sub>5</sub>
  • HY-W873806
    CRBN ligand-789 2304754-82-1
    CRBN ligand-789 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. CRBN ligand-789 can be linked to a target protein ligand via a linker to form a PROTAC.
    CRBN ligand-789
  • HY-W452755
    (R)-Desamino lenalidomide-5-Br 2243825-20-7 99.69%
    (R)-Desamino lenalidomide-5-Br is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. (R)-Desamino lenalidomide-5-Br can be linked to a target protein ligand via a linker to form a PROTAC.
    (R)-Desamino lenalidomide-5-Br
  • HY-W998252
    CRBN ligand-206 1486115-10-9
    CRBN ligand-206 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. CRBN ligand-206 can be linked to a target protein ligand via a linker to form a PROTAC.
    CRBN ligand-206
  • HY-W875713
    5-Fluoro-lenalidomide 1918158-58-3
    5-Fluoro-lenalidomide is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. 5-Fluoro-lenalidomide can be linked to a target protein ligand via a linker to form a PROTAC.
    5-Fluoro-lenalidomide
  • HY-W391701
    Pomalidomide-COCH2Cl 444287-84-7 98.52%
    Pomalidomide-COCH2Cl is a derivative of Pomalidomide with an chloroacetamide group on the benzyl ring.
    Pomalidomide-COCH2Cl
  • HY-W586331
    Thalidomide-iodo 2509137-01-1 98.0%
    Thalidomide-iodo is an iodinated E3 ligase activator. Thalidomide-iodo can be used for further derivitization by substitution of iodine.
    Thalidomide-iodo
  • HY-W589407
    Desamino lenalidomide-6-propyne 2412439-22-4
    Desamino lenalidomide-6-propyne is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. Desamino lenalidomide-6-propyne can be linked to a target protein ligand via a linker to form a PROTAC.
    Desamino lenalidomide-6-propyne
  • HY-W586821
    Thalidomide-1-Me-5-NH2 1468761-60-5 98.0%
    Thalidomide-1-Me-5-NH2 is an aminated Thalidomide analogue. E3 Ligase activators such as this may be used in the design of PROTAC molecules via derivatization at its amine.
    Thalidomide-1-Me-5-NH2
  • HY-W441271
    Deoxy-thalidomide-5-iodine 2291364-01-5 98.0%
    Deoxy-thalidomide-5-iodine is a Thalidomide analog that can be useful in PROTAC research.
    Deoxy-thalidomide-5-iodine
  • HY-W539393
    CRBN ligand-891 2618349-23-6
    CRBN ligand-891 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. CRBN ligand-891 can be linked to a target protein ligand via a linker to form a PROTAC.
    CRBN ligand-891
  • HY-W586342
    Desamino lenalidomide-COOH 2287259-68-9 98.58%
    Desamino lenalidomide-COOH is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. Desamino lenalidomide-COOH can be linked to a target protein ligand via a linker to form a PROTAC.
    Desamino lenalidomide-COOH
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