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-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
  • 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-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-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-46531
    Thalidomide-5-NH2-CH2-COOH 2412056-27-8
    Thalidomide-5-NH2-CH2-COOH (compound 114) is a potent and selective inhibitor of tropomyosin receptor kinase (trk). Thalidomide-5-NH2-CH2-COOH is a ligand of E3 ligase. Thalidomide-5-NH2-CH2-COOH has the potential for researching one or more diseases (extracted from patent WO2021170109A1).
    Thalidomide-5-NH2-CH2-COOH
  • HY-W076696
    Lenalidomide-4-OH 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.
    Lenalidomide-4-OH
  • HY-43961
    E3 ligase Ligand 8 1225383-33-4 99.32%
    E3 ligase Ligand 8 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 8 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
    E3 ligase Ligand 8
  • 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-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-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-143715
    Cereblon inhibitor 1 2672489-14-2 99.19%
    Cereblon inhibitor 1, an isoindoline derivative, is a cereblon E3 ubiquitin ligase modulating agent. Cereblon inhibitor 1 has the potential for cancer research.
    Cereblon inhibitor 1
  • HY-10984S1
    Pomalidomide-d3 2093128-28-8 ≥99.0%
    Pomalidomide-d3 is the deuterium labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors[1][2].
    Pomalidomide-d<sub>3</sub>
  • HY-47851
    VH 101, thiol 2358775-81-0
    VH 101, thiol (compound 20) is a VHL ligand for the synthesis of PROTACs.
    VH 101, thiol
  • HY-129653
    E3 ligase Ligand 18 2241669-88-3 99.22%
    E3 ligase Ligand 18 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 18 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
    E3 ligase Ligand 18
  • HY-131887
    Pomalidomide-C6-COOH 2225940-50-9 98.02%
    Pomalidomide-C6-COOH is the pomalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide-6-OH can be connected to the ligand for protein by a linker to form PROTAC.
    Pomalidomide-C6-COOH
  • HY-A0003S
    Lenalidomide-d5 1227162-34-6 99.32%
    Lenalidomide-d5 is deuterium labeled Lenalidomide. Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells[1][2].
    Lenalidomide-d<sub>5</sub>
  • HY-42424A
    (S,R,S)-AHPC-Me dihydrochloride 2504950-56-3 99.54%
    (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-W342590
    CRBN ligand-9 55003-81-1 ≥98.0%
    CRBN ligand-9 (Compound 4d) is a CRBN ligand (Ki: 8.9 μM). CRBN ligand-9 can be used for synthesis of PROTACs.
    CRBN ligand-9
  • HY-111823
    VH032 thiol 2098836-54-3
    VH032 thiol (VHL ligand 6) is a VHL ligand, which binds to pan-BET inhibitor JQ1 via a linker to form PROTAC.
    VH032 thiol
  • HY-138678
    (R,S,S)-VH032 2230826-33-0
    (R,S,S)-VH032 is Ligand for E3 Ligase used in the synthesis of PROTACs. VH032 is a VHL ligand and VHL/HIF-1α interaction inhibitor that recruits von Hippel-Lindau (VHL) proteins. (R,S,S)-VH032 synthesizes the tau-targeting small molecule PROTAC C004019 (HY-138669).
    (R,S,S)-VH032
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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