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-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-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-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-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-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-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-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-W1004786
    CRBN ligand-13 3050687-70-9
    CRBN ligand-13 is a CRBN-type E3 ubiquitin ligase ligand that can be used to prepare PROTAC.
    CRBN ligand-13
  • 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-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-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-133144
    Lenalidomide-OH 1416990-08-3 99.48%
    Lenalidomide-OH is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein. Lenalidomide-OH can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC BTK degrader SJF620 (HY-133137).
    Lenalidomide-OH
  • HY-114406
    TD-106 2250288-69-6 99.81%
    TD-106 is a cereblon (CRBN) modulator, which can be used for targeted protein degradation. BRD4 PROTACs with TD-106 induce BRD4 degradation.
    TD-106
  • HY-W023573
    5-Aminothalidomide 191732-76-0 99.69%
    5-Aminothalidomide is an E3 ligase ligand used in PROTAC technology. 5-Aminothalidomide can be used to synthesize various PROTACs, such as the PROTAC BRD9 Degrader-7 (HY-155361).
    5-Aminothalidomide
  • HY-111663
    VL285 1448188-57-5 99.34%
    VL285 is a potent VHL ligand with an IC50 of 0.34 μM.
    VL285
  • HY-131385
    KB02-COOH 2375196-30-6 99.39%
    KB02-COOH is a fragment of synthesis of ubiquitin E3 ligase ligand KB02. KB02 can be used in the synthesis of PROTAC, such as KB02-JQ1 (HY-129917) and KB02-SLF (HY-129610).
    KB02-COOH
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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