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  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
製品番号 製品名 CAS 番号 純度 構造式
  • HY-168293
    p62-ZZ ligand 1 2409960-13-8
    p62-ZZ ligand 1 (Compound 7) is an p62-ZZ ligand. p62-ZZ ligand 1 can be used for synthesis of VinclozolinM2-2204 (HY-161741).
    p62-ZZ ligand 1
  • HY-168536
    SJ46411 3086104-39-1
    SJ46411 is a potent ligand for KLHDC2, with a Kd of ~260 nM measured by isothermal titration calorimetry (SPR Kd = 0.5 μM, TR-FRET IC50 = 3.9 μM, ΔTm = 6.0 °C).
    SJ46411
  • HY-168055
    (S)-Deoxy-thalidomide 107657-57-8
    (S)-Deoxy-thalidomide is an E3 ubiquitin ligase ligand. (S)-Deoxy-thalidomide can be linked to the target protein ligand through a linker to form PROTAC K-Ras Degrader-3 (HY-168054). PROTAC K-Ras Degrader-3 can target KRAS mutant proteins for degradation.
    (S)-Deoxy-thalidomide
  • HY-111853
    MV-1-NH-Me 2095244-62-3
    MV-1-NH-Me, the MV-1 based IAP ligand, binds to ABL inhibitor via a linker to form SNIPER.
    MV-1-NH-Me
  • HY-128810
    E3 ligase Ligand 13 2701565-75-3
    E3 ligase Ligand 13 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 13 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 13
  • HY-132944
    (R)-Pomalidomide-pyrrolidine 2418618-52-5
    (R)-Pomalidomide-pyrrolidine, a CRBN ligand, can be connected to the ligand for protein by a linker to form PROTACs.
    (R)-Pomalidomide-pyrrolidine
  • HY-112078A
    (S,R,S,R)-AHPC-Me 2055344-67-5
    (S,R,S,R)-AHPC-Me serves as a VHL ligand that facilitates the recruitment of the VHL protein.
    (S,R,S,R)-AHPC-Me
  • HY-172563
    BTR2000
    BTR2000, a specifically KLHL20 ligand, is capable of binding to the KLHL20 Kelch domain with high affinity. BTR2000 can be used as a ligand for E3 ligase for the synthesis of BTR2004 (HY-172562).
    BTR2000
  • HY-45808
    Thalidomide-azetidine-CHO 2416132-70-0
    Thalidomide-azetidine-CHO is a synthesized Ligands for E3 Ligase that incorporates the Thalidomide (HY-14658) based cereblon ligand used in PROTAC technology.
    Thalidomide-azetidine-CHO
  • HY-169147
    MY-11B 2929223-25-4
    MY-11B is a DCAF1 ligand. MY-11B shows reactivity with DCAF1_C1113. MY-11B blockes YT41R and YT47R-mediated degradation of HA-FKBP12. MY-11B can be used in the synthesis of PROTACs.
    MY-11B
  • HY-161668
    Ru-Poma
    Ru-Poma is a Ru(II)-based photosensitizer, which attenuates Cisplatin (HY-17394)-resistant tumor through photodynamic therapy (PDT). Ru-Poma photodegrades CRBN through a Pomalidomide (HY-10984) moiety. Ru-Poma induces ferroptosis, through an increase in lipid peroxide, downregulation of GPX4 and GAPDH expression. Ru-Poma exhibits cytotoxicity in A549, with IC50 of 18.46 μM and 0.37 μM in dark and upon irradiation, respectively.
    Ru-Poma
  • HY-176804
    (R,S,R)-AHPC-Me-Ac
    (R,S,R)-AHPC-Me-Ac is an E3 ligase ligand used in the synthesis of the PROTAC SHP2 Protein degrader-2 (HY-145703).
    (R,S,R)-AHPC-Me-Ac
  • HY-168699
    E3 ligase Ligand 45
    E3 ligase Ligand 45 is an E3 ligase ligand that can be used to synthesize the PROTAC degrader Setidegrasib (HY-148273) for Ras.
    E3 ligase Ligand 45
  • HY-W584527
    VH032 analogue-1 2111829-84-4
    VH032 analogue-1 is a VH032 (HY-120217) analog that acts as a ligand for VHL, recruiting von Hippel-Lindau (VHL) protein. VH032 analogue-1 will remove the protective group under acidic conditions and be directly used for PROTAC molecular synthesis. VH032 analogue-1 is a key intermediate in the synthesis of PROTACs based on VHL ligands.
    VH032 analogue-1
  • HY-173627A
    (R,S,S)-VH032-Me TFA 2451573-93-4
    (R,S,S)-VH032-Me TFA is an E3 ligase Ligand and can be used for synthesis of dTAGV-1 hydrochloride (HY-145514C).
    (R,S,S)-VH032-Me TFA
  • HY-161415
    BCL-xL/BCL-2 ligand 1 2941091-91-2
    BCL-xL/BCL-2 ligand 1 (compound 72-1) is a BCL-xL and BCL-2 protein ligand. BCL-xL/BCL-2 ligand 1 can be connected to the E3 ligase by a linker to form PROTACs (HY-161410).
    BCL-xL/BCL-2 ligand 1
  • HY-181591
    IAP ligand 10
    IAP ligand 10 is an E3 ligase ligand (E3 ligase ligand). E3 ligase Ligand 58 can be used for the synthesis of PROTAC TEAD1/IAP degrader-3 (HY-181590).
    IAP ligand 10
  • HY-161770
    HL389
    HL389 inhibits proliferation of cancer cells MDA-MB-231 and MCF-7, with IC50 of 11.39 μM and 9.66 μM. HL389 can be utilized as the ligand for E3 ligase for the synthesis of PROTAC degrader HL435 (HY-161769).
    HL389
  • HY-139549
    Thalidomide-benzo 458151-34-3
    Thalidomide-benzo hydrochloride is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-benzo can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-benzo
  • HY-W797329
    (3S)Lenalidomide-5-Br 2829898-76-0 98.61%
    (3S)Lenalidomide-5-Br is a ligand for E3 ubiquitinase. (3S)Lenalidomide-5-Br can be used to synthesize PROTAC Cbl-b-IN-1 (HY-159608).
    (3S)Lenalidomide-5-Br
製品番号 製品名 / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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