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-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-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-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-139539
    Thalidomide-5-COOH 1216805-11-6 99.97%
    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-149934
    DCAF1 binder 1 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-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-156106
    VHL-IN-1 3033117-53-9 99.78%
    VHL-IN-1 (compound 30) is a ubiquitin E3 ligase von Hippel-Lindau (VHL) inhibitor (dissociation constant Kd=37 nM) that stabilizes and induces HIF-1α transcriptional activity. VHL-IN-1 has potential as a HIF-1α stabilizer and degrader of proteolytically targeted chimeras (PROTACs).
    VHL-IN-1
  • HY-145152
    Biotin-Thalidomide 2230857-87-9 99.65%
    Biotin-Thalidomide is a cereblon affinity probe for PROTAC and targeted protein degradation research.
    Biotin-Thalidomide
  • 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-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-114406
    TD-106 2250288-69-6 98.67%
    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-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-130845A
    AR antagonist 1 hydrochloride 1818885-55-0 99.53%
    AR antagonist 1 (compound 29) hydrochloride 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 hydrochloride
  • HY-123215
    CC-17369 1547162-46-8 98.13%
    CC-17369 (7-Hydroxy pomalidomide) is a metabolite of Pomalidomide. CC-17369 is the Pomalidomide -based cereblon (CRBN) ligand used in the recruitment of CRBN protein. CC-17369 can be connected to the ligand for protein by a linker to form PROTAC.
    CC-17369
  • 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-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
  • 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-W761299
    PD 4'-oxyacetic acid 2633633-12-0 99.69%
    PD 4'-oxyacetic acid is a carboxylic acid-functionalized cereblon ligand that can be used for PROTAC Degrader development.
    PD 4'-oxyacetic acid
  • HY-47851
    VH 101, thiol 2358775-81-0 98.66%
    VH 101, thiol (compound 20) is a VHL ligand for the synthesis of PROTACs.
    VH 101, thiol
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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