2. Signaling Pathways
  3. PROTAC
  4. Ligands for E3 Ligase

Ligands for E3 Ligase

E3 ligase-recruiting Moiety

Ligands for E3 Ligase

Related Products

PDF 1.28 MB

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-163932
    (S,R,S)-AHPC-O-CF3 2641373-92-2
    (S,R,S)-AHPC-O-CF3 is a ligand for E3 ubiquitinase. (S,R,S)-AHPC-O-CF3 can be used to synthesize PROTAC SMARCA2/4-degrader-20 (HY-163873).
    (S,R,S)-AHPC-O-CF3
  • HY-101763B
    (S,R,S)-AHPC dihydrochloride 2137142-47-1
    (S,R,S)-AHPC (VH032-NH2) dihydrochloride is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC dihydrochloride 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 dihydrochloride
  • HY-168232
    E3 ligase Ligand 35
    E3 ligase Ligand 35 serves as the E3 ligase ligand for PROTAC SMARCA2 degrader-27 (HY-168229).
    E3 ligase Ligand 35
  • HY-168646
    SJ46411-Br
    SJ46411-Br is one of CRL2KLHDC2 targeting Ligands for E3 Ligase. SJ46411-Br can bind to KLHDC2 to form a complex to promote cooperative homologous selective ternary complex formation. SJ46411-Br can be coupled to BET ligand JQ1 (HY-13030) through PROTAC linker to synthesize corresponding PROTACs.
    SJ46411-Br
  • HY-401613
    E3 ligase Ligand 43 2821795-71-3
    E3 ligase Ligand 43 serves as the E3 ubiquitin ligase ligand for ACBI3 (HY-157228). E3 ligase Ligand 43 can be utilized for the synthesis of PROTACs.
    E3 ligase Ligand 43
  • HY-159076
    E3 ligase Ligand 7 37630-54-9
    E3 ligase Ligand 7 (Compound 6) is a ligand for E3 ligase. E3 ligase Ligand 7 can be utilized for the synthesis of PROTAC BET Degrader-12 (HY-158764).
    E3 ligase Ligand 7
  • HY-157749
    Thalidomide-piperazine-(S)-CH2-pyrrolidine-C2-O-CH2-COO-C(CH3)3
    Thalidomide-piperazine-(S)-CH2-Pyrrolidine-C2-O-CH2-COO-C (CH3)3 is a synthetic E3 ligase ligand-Linker conjugate. Thalidomide-piperazine-(S)-Ch2-Pyrrolidine-C2-O-CH2-COO-C(CH3)3 includes Thalidomide-based cereblon ligands and linkers. Thalidomide-piperazine-(S)-CH2-Pyrrolidine-C2-O-CH2-COO-C(CH3)3 can be used to synthesize PROTAC BET.
    Thalidomide-piperazine-(S)-CH2-pyrrolidine-C2-O-CH2-COO-C(CH3)3
  • HY-175343A
    OICR-41103N
    OICR-41103N is the negative control form of OICR-41103 (HY-175343). OICR-41103 is an effective, selective, cell-active DCAF1 small molecule chemical probe (Ki<2 nM) that targets the DCAF1 WDR domain and replaces the viral Vpr protein.
    OICR-41103N
  • 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-161195
    Deoxy-thalidomide-piperidine-C-piperazine-C-boc
    Deoxy-thalidomide-piperidine-C-piperazine-C-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Deoxy-thalidomide-piperidine-C-piperazine-C-boc can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Deoxy-thalidomide-piperidine-C-piperazine-C-boc
  • 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-W733888
    CRBN ligand-187 2883704-28-5
    CRBN ligand-187 is a CRBN-type E3 ubiquitin ligase ligand that can be used for synthesis of TQ-3959 (HY-175541).
    CRBN ligand-187
  • 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-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
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.