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-125845
    (S,R,S)-AHPC 1448297-52-6 99.13%
    (S,R,S)-AHPC (VH032-NH2) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC 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
  • HY-117937
    BC-1215 1507370-20-8 99.93%
    BC-1215 is a F-box protein 3 (Fbxo3) inhibitor. BC-1215 works by antagonizing of Fbxo3 on TRAF cytokine signaling and exhibits a low IC50 in vitro. BC-1215 can be used for the research of inflammation.
    BC-1215
  • HY-145776
    ALV1 2438124-79-7
    ALV1 potently induces degradation of both Ikaros and Helios without unexpected off-target activity. ALV1 binds CRBN with IC50 of 0.55 µM. ALV1 degrades cells stably expressing IKZF1Δ and IKZF2Δ GFP fusions with mCherry reporter with DC50s of 2.5 and 10.3 nM.
    ALV1
  • 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-111663
    VL285 1448188-57-5 98.84%
    VL285 is a potent VHL ligand with an IC50 of 0.34 μM.
    VL285
  • HY-W072954
    Lenalidomide-5-Br 1010100-26-1 99.00%
    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-126456
    (S,R,S)-AHPC-propargyl 2098799-78-9 99.48%
    (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-112078
    (S,R,S)-AHPC-Me 1948273-02-6 98.70%
    (S,R,S)-AHPC-Me (VHL ligand 2) 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 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
  • HY-14658A
    (S)-Thalidomide 841-67-8 99.65%
    (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-133045
    VHL Ligand 8 2701565-76-4 99.71%
    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-114406
    TD-106 2250288-69-6 99.17%
    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-128837
    Nutlin carboxylic acid 2249750-27-2 98.36%
    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-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
  • HY-152231
    BODIPY FL thalidomide 2740620-18-0 99.20%
    BODIPY FL thalidomide is a high-affinity fluorescent probe for the human cereblon protein with a Kd value of 3.6 nM[1]
    BODIPY FL thalidomide
  • HY-125292
    NV03 2448341-58-8 98.82%
    NV03 is a potent and selective antagonist of UHRF1 (Ubiquitin-like with PHD and RING finger domains 1)- H3K9me3 interaction by binding to UHRF1 tandem tudor domain, with a Kd of 2.4 μM. NV03 has anticancer activity.
    NV03
  • 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-136164
    VH032-OH 2244684-42-0 99.43%
    VH032-OH is the VH032-based VHL ligand. VH032-OH can be connected to the ligand for protein by a linker to form PROTACs.
    VH032-OH
  • HY-133699
    Pomalidomide-PEG4-COOH 2138440-81-8 ≥98.0%
    Pomalidomide-PEG4-COOH is a E3 ligase ligand-linker conjugate. Pomalidomide-PEG4-COOH contains the Pomalidomide based cereblon ligand and 4-unit PEG linker used in PROTAC technology (extracted from patent WO2017184995A1).
    Pomalidomide-PEG4-COOH
  • HY-W077589
    Lenalidomide-5-aminomethyl hydrochloride 1158264-69-7 98.77%
    Lenalidomide-5-aminomethyl hydrochloride is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-5-aminomethyl hydrochloride can be connected to the ligand for protein by a linker to form PROTAC
    Lenalidomide-5-aminomethyl hydrochloride
  • HY-138040
    CRBN modulator-1 2407829-65-4 98.06%
    CRBN modulator-1, a Thalidomide analog and a CRBN modulator extracted from WO2020006262A1, compound 10, has an IC50 of 3.5 μM and a Ki of 0.98 μM.
    CRBN modulator-1
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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