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-130949B
    Thalidomide-4-O-C7-NH2 hydrochloride 99.80%
    Thalidomide-4-O-C7-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-4-O-C7-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-4-O-C7-NH2 hydrochloride
  • HY-14658B
    (R)-Thalidomide 2614-06-4 99.80%
    (R)-Thalidomide ((R)-(+)-Thalidomide) is the R-enantiomer of Thalidomide. (R)-Thalidomide has psychomotor stabilizing properties.
    (R)-Thalidomide
  • HY-A0003A
    Lenalidomide hydrochloride 1243329-97-6
    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-130845
    AR antagonist 1 1818885-54-9
    AR antagonist 1 (compound 29) is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020).
    AR antagonist 1
  • HY-110402
    (S,R,S)-AHPC TFA 1631137-51-3
    (S,R,S)-AHPC (VH032-NH2) TFA is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC TFA can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells.
    (S,R,S)-AHPC TFA
  • HY-10984S2
    Pomalidomide-d4 1416575-78-4
    Pomalidomide-d4 is the deuterium labeled Pomalidomide. 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-d<sub>4</sub>
  • HY-161185
    Thalidomide-piperidine-O-azetidine-boc 2991611-55-1
    Thalidomide-piperidine-O-azetidine-boc is a conjugate of E3 ubiquitin ligase ligand-Linker, which can be used to synthesize complete PROTACs molecules.
    Thalidomide-piperidine-O-azetidine-boc
  • HY-157758
    (S)-Thalidomide-piperazine-pyrimidine-piperazine-C2-O-CH2-COO-C(CH3)3
    (S)-Thalidomide-piperazine-pyrimidine-piperazine-C2-O-CH2-COO-C(CH3)3 is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker . (S)-Thalidomide-piperazine-pyrimidine-piperazine-C2-O-CH2-COO-C(CH3)3 can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    (S)-Thalidomide-piperazine-pyrimidine-piperazine-C2-O-CH2-COO-C(CH3)3
  • HY-W077589A
    Lenalidomide-5-aminomethyl 1010100-28-3
    Lenalidomide-5-aminomethyl is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-5-aminomethyl can be connected to the ligand for protein by a linker to form PROTAC.
    Lenalidomide-5-aminomethyl
  • HY-161467
    Aster-A Ligand-3 2375541-28-7
    Aster-A Ligand-3 is a target protein ligand and can be used to synthesize PROTAC Aster-A degrader (HY-D2336).
    Aster-A Ligand-3
  • HY-161199
    Thalidomide-azetidine-pyrrolidine-C-piperidine-C2-OH
    Thalidomide-azetidine-pyrrolidine-C-piperidine-C2-OH is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-azetidine-pyrrolidine-C-piperidine-C2-OH can serve as Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Thalidomide-azetidine-pyrrolidine-C-piperidine-C2-OH
  • HY-161639
    E3 ligase Ligand 26 2911613-35-7
    E3 ligase Ligand 26 (part of Compd 10) is a ligand for E3 ligase, used for the synthesis of PROTAC SOS1 degrader (HY-161636).
    E3 ligase Ligand 26
  • HY-128806
    E3 ligase Ligand 9 87304-15-2
    E3 ligase Ligand 9 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 9 can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
    E3 ligase Ligand 9
  • HY-161210
    Thalidomide-azetidine-C-PIP-C-boc 2589699-87-4
    Thalidomide-azetidine-C-PIP-C-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-azetidine-C-PIP-C-boc can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Thalidomide-azetidine-C-PIP-C-boc
  • HY-161193
    Thalidomide-piperazine-(R)-C-pyrrolidine-C-boc
    Thalidomide-piperazine-(R)-C-pyrrolidine-C-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-piperazine-(R)-C-pyrrolidine-C-boc can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Thalidomide-piperazine-(R)-C-pyrrolidine-C-boc
  • HY-161200
    Thalidomide-piperazine-C-azetidine-C2-OH
    Thalidomide-piperazine-C-azetidine-C2-OH is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-piperazine-C-azetidine-C2-OH can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Thalidomide-piperazine-C-azetidine-C2-OH
  • HY-144983
    E3 ligase Ligand 22 2377849-57-3
    E3 ligase Ligand 22 (compound 139) is a cereblon binder for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway.
    E3 ligase Ligand 22
  • HY-162035
    MDM2-IN-23
    MDM2-IN-23 (compound 5d) is an inhibitor of MDM2. MDM2-IN-23 has an IC50 of 60.09 μM on MCF-7 cells.
    MDM2-IN-23
  • HY-139541
    Pomalidomide-5-O-CH3 1547163-02-9
    Pomalidomide-5-O-CH3 is the Pomalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide-5-O-CH3 can be connected to the ligand for protein by a linker to form PROTAC.
    Pomalidomide-5-O-CH3
  • HY-W584515
    Thalidomide-NH-(CH2)3-NH-Boc 2093386-36-6
    Thalidomide-NH-(CH2)3-NH-Boc is a Boc-modified Thalidomide (HY-14658), which acts as a Cereblon ligand to recruit CRBN protein. The Boc protecting group at the end of Thalidomide-NH-(CH2)3-NH-Boc can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-NH-(CH2)3-NH-Boc is a key intermediate in the synthesis of CRBN-based designed PROTAC molecules targeting 11β-substituted estradiol.
    Thalidomide-NH-(CH2)3-NH-Boc
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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