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-131318
    Lenalidomide-I 2207541-30-6 99.90%
    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-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-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-128808
    cIAP1 ligand 1 2095244-42-9 99.90%
    cIAP1 ligand 1 is the LCL161 derivative based IAP ligand. cIAP1 ligand 1 can be connected to the ABL ligand for protein by a linker to form SNIPER. cIAP1 ligand 1 can be used in prostate cancer research.
    cIAP1 ligand 1
  • 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-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-128837
    Nutlin carboxylic acid 2249750-27-2 98.63%
    Nutlin carboxylic acid (MDM2 ligand 1) is the Nutlin 3-based MDM2 ligand. Nutlin carboxylic acid can be connected to the ligand for protein by a linker to form PROTAC.
    Nutlin carboxylic acid
  • HY-W460193
    N-Me-Thalidomide 4-fluoride 2244520-92-9 99.41%
    N-Me-Thalidomide 4-fluoride is a ligand for E3 ligase, used for the synthesis of Anti-inflammatory agent 70 (HY-157570).
    N-Me-Thalidomide 4-fluoride
  • HY-139539
    Thalidomide-5-COOH 1216805-11-6 99.94%
    Thalidomide-5-COOH is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-COOH can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-COOH
  • HY-126456
    (S,R,S)-AHPC-propargyl 2098799-78-9 99.46%
    (S,R,S)-AHPC-propargyl (VH032-propargyl) is a VHL ligand which is used in “click reaction” for PROTACs. (S,R,S)-AHPC-propargyl is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    (S,R,S)-AHPC-propargyl
  • 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-133045
    VHL Ligand 8 2701565-76-4 98.04%
    VHL Ligand 8 is a VHL ligand. VHL Ligand 8 can be used to synthesize ARD-266 (HY-133020), a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM.
    VHL Ligand 8
  • HY-W093272
    Thalidomide-5,6-F 1496997-41-1 99.84%
    Thalidomide-5,6-F is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5,6-F can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5,6-F
  • HY-111663
    VL285 1448188-57-5 99.34%
    VL285 is a potent VHL ligand with an IC50 of 0.34 μM.
    VL285
  • HY-138881
    Lenalidomide-6-F 2468780-87-0 99.63%
    Lenalidomide-6-F is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-6-F can be connected to the ligand for protein by a linker to form PROTAC.
    Lenalidomide-6-F
  • HY-14658R
    Thalidomide (Standard) 50-35-1
    Thalidomide (Standard) is the analytical standard of Thalidomide. This product is intended for research and analytical applications. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ∼250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide can work as molecular glue to potentiate substrate.
    Thalidomide (Standard)
  • HY-123109
    (S,R,S)-AHPC-Boc 1448189-98-7
    (S,R,S)-AHPC-Boc (VH032-Boc) is a ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Boc is used in PROTAC technology.
    (S,R,S)-AHPC-Boc
  • HY-150803
    VHL Ligand 14 2010986-87-3 99.93%
    VHL Ligand 14 (Compound 11) is a VHL ligand for design of PROTAC estrogen receptor α (ERα) degraders, with a binding affinity IC50 of 196 nM.
    VHL Ligand 14
  • HY-W076696
    3-(4-Hydroxy-1-oxoisoindolin-2-yl)piperidine-2,6-dione 1061604-41-8 98.57%
    Lenalidomide-4-OH is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-4-OH can be connected to the ligand for protein by a linker to form PROTAC.
    3-(4-Hydroxy-1-oxoisoindolin-2-yl)piperidine-2,6-dione
  • HY-42424A
    (S,R,S)-AHPC-Me dihydrochloride 2504950-56-3 99.84%
    (S,R,S)-AHPC-Me dihydrochloride (VHL ligand 2 dihydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me dihydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM.
    (S,R,S)-AHPC-Me dihydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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