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-169968
    E3 ligase Ligand 41 2375196-68-0
    E3 ligase Ligand 41 (Compound SI-13) is a ligand for E3 ubiquitin ligase DCAF16. E3 ligase Ligand 41 can be connected to SLF (HY-114872) by a linker (HY-W040168) to form KB03-SLF (HY-147196).
    E3 ligase Ligand 41
  • HY-168280
    AS1411-C4-VH032
    AS1411-C4-VH032 (AS1411-VH032) promotes tumor-selective degradation of MDM2, leading to tumor shrinkage without detectable toxicity.
    AS1411-C4-VH032
  • HY-174401
    PROTAC HDAC6 degrader 5
    PROTAC HDAC6 degrader 5 (Compound 5a) is a highly selective PROTAC targeting HDAC6. PROTAC HDAC6 degrader 5 can effectively degrade HDAC6 in cells (IC50 = 43 nM). PROTAC HDAC6 degrader 5 reduces HDAC6 levels through proteasome- and CRBN-dependent mechanisms (Pink: Target protein ligand (HY-174408), Target protein ligand + linker (HY-174409); Blue: Pomalidomide (HY-10984), Pomalidomide 4'-alkylC3-azide (HY-139341)).
    PROTAC HDAC6 degrader 5
  • HY-176917
    E3 ligase Ligand 76
    E3 ligase Ligand 76 is a E3 ligase ligand that can be used in the recruitment of VHL protein. E3 ligase Ligand 76 can be connected to the KRAS ligand (HY-162960) by a linker to synthesis of PROTAC KRAS(on) degrader ACBI-4 (HY-176792).
    E3 ligase Ligand 76
  • HY-161367
    VHL-SF2 3050690-24-6
    VHL-SF2 is a VHL ligand, and can be used for synthesis of PROTACs
    VHL-SF2
  • HY-128809
    cIAP1 ligand 2 2357114-70-4
    cIAP1 ligand 2 is the LCL161 derivative based IAP ligand. cIAP1 ligand 2 can be connected to the ABL ligand for protein by a linker to form SNIPER.
    cIAP1 ligand 2
  • HY-170826
    SMARCA2 ligand-14
    SMARCA2 ligand-14 is the ligand for SMARCA2 that can be used for synthesis of PROTAC degrader SMD-3236 (HY-170824).
    SMARCA2 ligand-14
  • HY-168865
    E3 ligase Ligand 53
    E3 ligase Ligand 53 is a FEM1B ligand used to recruit Fem-1 homologue B (FEM1B) proteins. E3 ligase Ligand 53 can be attached to target protein ligands (e.g. HDAC1) via a linker to form PROTAC molecules (e.g. FF2049).
    E3 ligase Ligand 53
  • HY-169359
    L321
    4-Methylphenoxyacetic acid-Oxindole-CF3 is the E3 ligase ligand part of L134 (HY-169358). 4-Methylphenoxyacetic acid-Oxindole-CF3 can be utilized in PROTAC synthesis.
    L321
  • HY-150799
    CRBN ligand-1 3032314-67-0
    CRBN ligand-1 is a ligand for E3 ligase.
    CRBN ligand-1
  • HY-175348
    XB2M54 1467165-30-5
    XB2M54 is a selective XIAP antagonist. XB2M54 inhibits NOD2-mediated inflammatory signaling. XB2M54 is an E3 ligase ligand. XB2M54 can be used for synthesis of PROTAC ERα Degrader-1 (HY-112098).
    XB2M54
  • HY-139547
    Thalidomide-5,6-Cl 2648939-40-4
    Thalidomide-5,6-Cl is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5,6-Cl can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5,6-Cl
  • HY-178517
    Thalidomide-C1-O-CO-C11
    Thalidomide-C1-O-CO-C11 is a ligand for E3 ubiquitin ligase. Thalidomide-C1-O-CO-C11 can be connected to Aurora-A ligand 1 (HY-168440) by a linker (HY-178512) to form PROTAC CDK4/6/9 degrader 2 (HY-178516).
    Thalidomide-C1-O-CO-C11
  • HY-139656
    cIAP1 ligand 4 2891589-73-2
    cIAP1 ligand 4 is a ligand for E3 ligase that can be used in the synthesis of PROTACs.
    cIAP1 ligand 4
  • HY-170671
    E3 ligase Ligand 49 1911013-66-5
    E3 ligase Ligand 49 serves as the E3 ubiquitin ligase ligand for PROTAC XPO1 degrader-1 (HY-170669). E3 ligase Ligand 49 can be utilized for the synthesis of PROTACs.
    E3 ligase Ligand 49
  • HY-175654
    6-(2,4-Dioxopyrimidin-1-yl)-1-methylindole 2766178-76-9
    6-(2,4-Dioxopyrimidin-1-yl)-1-methylindole is an E3 ligase ligand used in the synthesis of the PROTAC Androgen receptor degrader-1 (HY-175652).
    6-(2,4-Dioxopyrimidin-1-yl)-1-methylindole
  • HY-139542
    Pomalidomide-6-O-CH3 1547163-08-5
    Pomalidomide-6-O-CH3 is the Pomalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide-6-O-CH3 can be connected to the ligand for protein by a linker to form PROTAC.
    Pomalidomide-6-O-CH3
  • HY-163927
    E3 ligase Ligand 29 2154341-52-1
    E3 ligase Ligand 29 is a ligand for E3 ligase.
    E3 ligase Ligand 29
  • HY-180993
    CRBN ligand-894
    CRBN ligand-894 (Compound 8) is an E3 ubiquitin ligase ligand for cereblon (CRBN), with a KD value of 188 nM. CRBN ligand-880 can be linked to the target protein ligand through a linker to form a PROTAC.
    CRBN ligand-894
  • HY-182008
    NEURL1B-IN-1 3068938-30-4
    NEURL1B-IN-1 is a molecular glue-like NEURL1B degrader with a Kd value of 46.2 nM. NEURL1B-IN-1 binds to Arg422 within the NHR2 domain of NEURL1B, triggers its autoubiquitination and proteasomal degradation, disrupts its interaction with DLL1, and attenuates the Notch signaling pathway. NEURL1B-IN-1 induces cell cycle arrest and apoptosis, and inhibits migration of hepatocellular carcinoma cells. NEURL1B-IN-1 is applicable to research related to hepatocellular carcinoma.
    NEURL1B-IN-1
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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