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-170126S
    9-Amino-1,2,3,4-tetrahydroacridin-1-ol-d3 Maleate 1219806-48-0
    9-Amino-1,2,3,4-tetrahydroacridin-1-ol-d3 Maleate is the deuterium labeled CRBN ligand-74 (HY-170126). CRBN ligand-74 is a CRBN-type E3 ubiquitin ligase ligand that can be used to prepare PROTAC.
    9-Amino-1,2,3,4-tetrahydroacridin-1-ol-d<sub>3</sub> Maleate
  • HY-W454906
    tDHU, acid 2377643-37-1 98.83%
    tDHU, acid is a dihydropyrimidinecereblon ligand that contains an E3 ligase ligand and a benzoic acid linker. tDHU, acid can be used as an E3 ubiquitin ligase ligand-Linker conjugate for the development of PROTACs.
    tDHU, acid
  • HY-W890189
    E3 ligase Ligand 54 2413038-90-9
    E3 ligase Ligand 54 is the ligand for E3 ligase Cereblon and can be used for synthesis of PROTAC Degrader SJ44236 (HY-170900).
    E3 ligase Ligand 54
  • HY-157558
    KDRLKZ-1
    KDRLKZ-1 is a KLHDC2 ligand (Kd = 0.36 μM), with IC50s of 0.21 μM and 0.31 μM in alphaLISA and time-resolved fluorescence resonance energy transfer (TR-FRET) displacement assays.
    KDRLKZ-1
  • HY-161203
    Thalidomide-azetidine-piperazine-C2-O-C-boc
    Thalidomide-azetidine-piperazine-C2-O-C-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-azetidine-piperazine-C2-O-C-boc can serve as Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Thalidomide-azetidine-piperazine-C2-O-C-boc
  • HY-161208
    Deoxy-thalidomide-Pip-C-PIP-boc 2963655-14-1
    Deoxy-thalidomide-Pip-C-PIP-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Deoxy-thalidomide-Pip-C-PIP-boc can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Deoxy-thalidomide-Pip-C-PIP-boc
  • HY-163210
    Pomalidomide 5'-fluoro-6'-piperazine-4-methylpiperidine hydrochloride 2758431-94-4
    Pomalidomide 5'-fluoro-6'-piperazine-4-methylpiperidine hydrochloride (ZJT1) is an E3 ubiquitin ligase cereblon based on Pomalidomide (HY-10984) (CRBN) ligand for recruitment of cereblon protein. Pomalidomide 5'-fluoro-6'-piperazine-4-methylpiperidine hydrochloride can be linked to protein ligand by linker to form PROTAC.
    Pomalidomide 5'-fluoro-6'-piperazine-4-methylpiperidine hydrochloride
  • HY-161192
    Thalidomide-O-C4H4-N(Me)-piperidine-C-boc
    Thalidomide-O-C4H4-N(Me)-piperidine-C-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-O-C4H4-N(Me)-piperidine-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-O-C4H4-N(Me)-piperidine-C-boc
  • HY-171862
    Nef ligand-2 3066896-28-1
    Nef ligand-2 is a binder of Nef. Nef ligand-2 is Ligands for E3 Ligase. Nef ligand-2 is the Nef Binder portion of FC-14369 (HY-171860).
    Nef ligand-2
  • HY-163225
    (S)-Thalidomide-piperazine-(1S,4r)-cyclohexane-NH-Boc
    (S)-Thalidomide-piperazine-(1S,4r)-cyclohexane-NH-Boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. (S)-Thalidomide-piperazine-(1S,4r)-cyclohexane-NH-Boc 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-(1S,4r)-cyclohexane-NH-Boc
  • HY-168226
    E3 ligase Ligand 34 2931870-73-2
    E3 ligase Ligand 34 is the E3 ligase ligand part of PROTAC SMARCA2/4-degrader-35 (HY-168225) and can be utilized in the synthesis of PROTACs.
    E3 ligase Ligand 34
  • HY-161205
    Thalidomide-PIP-(R)C-pyrrolidine-boc 2839668-87-8
    Thalidomide-PIP-(R)C-pyrrolidine-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-PIP-(R)C-pyrrolidine-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-PIP-(R)C-pyrrolidine-boc
  • HY-W245311
    E3 ligase Ligand 51 2703915-71-1
    E3 ligase Ligand 51 is the ligand for E3 ligase CRBN that can be used for synthesis of PROTAC BTK Degrader-12 (HY-170413).
    E3 ligase Ligand 51
  • HY-W247437
    E3 ligase Ligand 56 1472731-41-1
    E3 ligase Ligand 56 is the ligand for E3 ligase Cereblon and can be used for syntheisis of PROTAC CDK9 degrader-11 (HY-170978).
    E3 ligase Ligand 56
  • HY-161184
    Deoxy-thalidomide-piperidine-C-piperazine-C2-OH
    Deoxy-thalidomide-piperidine-C-piperazine-C2-OH is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Deoxy-thalidomide-piperidine-C-piperazine-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.
    Deoxy-thalidomide-piperidine-C-piperazine-C2-OH
  • HY-159973
    Me-SJ46411
    Me-SJ46411 is an E3 ubiquitin ligase ligand, which can be used for the synthesis of PROTAC molecules. For example, Me-SJ46411 combined with PROTAC linker Boc-Piperazine-OH (HY-20797) and target protein ligand (+)-JQ-1 (HY-13030) can be used to synthesize the selective BRD3 PROTAC degrader SJ46420 (HY-168635)..
    Me-SJ46411
  • HY-148106
    MEL23 642072-49-9
    MEL23 is a MDM2 E3 ligase inhibitor that blocks the E3 ligase activity of the MDM2-MDMX complex. MEL23 inhibits Mdm2 and p53 ubiquitination in cells, reduce viability of cells with wild-type p53. MEL23 stabilizes MDM2 via a mechanism independent of p53 transcription.
    MEL23
  • HY-174994
    JY-5
    JY-5 is an E3 ligase ligand. JY-5 can be used for synthesis of PROTAC JY-21 (HY-174975).
    JY-5
  • HY-169390
    OICR-8268-acrylic acid
    OICR-8268-acrylic acid is a ligand for E3 ubiquitin ligase. OICR-8268-acrylic acid can be connected to the ligand for protein by a linker to form OICR41114 (HY-169389). OICR41114 can be used in anti-cancer research.
    OICR-8268-acrylic acid
  • HY-W1009348
    RR-11055 3026009-09-3
    RR-11055 (Compound 8) is a ligand for E3 ligase, that exhibits an affinity with cereblon with Ki of 0.38 μM. RR-11055 can be used for synthesis of PROTAC Degrader ERD-1233 (HY-169367).
    RR-11055
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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