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-122542A
    PPACK dihydrochloride 82188-90-7 99.07%
    PPACK dihydrochloride is an orally active, selective molecular glue degrader targeting IKZF2. Through a molecular glue mechanism, PPACK dihydrochloride binds to CRBN, recruits IKZF2 to form a ternary complex, and promotes its ubiquitination and proteasomal degradation. This further converts inhibitory regulatory T cells (Treg) into effector-like T cells, enhances CD8+ T cell responses, and modulates the Teff:Treg balance. PPACK dihydrochloride also increases the production of the inflammatory cytokine IL-2 and reduces the suppressive activity of Treg. PPACK dihydrochloride can be used in cancer immunotherapy research, and exhibits a synergistic effect when combined with immune checkpoint inhibitors such as anti-PD1.
    PPACK dihydrochloride
  • HY-A0003R
    Lenalidomide (Standard) 191732-72-6
    Lenalidomide (Standard) is the analytical standard of Lenalidomide. This product is intended for research and analytical applications. 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.
    Lenalidomide (Standard)
  • HY-W244657
    3-(6-Amino-1-oxoisoindolin-2-yl)piperidine-2,6-dione 191732-74-8 98.89%
    3-(6-Amino-1-oxoisoindolin-2-yl)piperidine-2,6-dione is a Lenalidomide analog that can be useful in PROTAC research because it is applicable to the recruitment of the CRBN protein.
    3-(6-Amino-1-oxoisoindolin-2-yl)piperidine-2,6-dione
  • HY-W440230
    5,6-Difluoro-desamino lenalidomide 2438241-40-6 98.94%
    5,6-Difluoro-desamino lenalidomide is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. 5,6-Difluoro-desamino lenalidomide can be linked to a target protein ligand via a linker to form a PROTAC.
    5,6-Difluoro-desamino lenalidomide
  • HY-W181530
    NCT02 790245-61-3 98.14%
    NCT02 is a molecular glue degrader based on the E3 ubiquitin ligase DDB1 that targets CDK12 and its binding partner CCNK. NCT02 triggers the ubiquitination and proteasomal degradation of CCNK, thereby downregulating CDK12 protein levels and inhibiting its downstream signaling pathways. NCT02 can induce tumor cell apoptosis, arrest the cell cycle, and selectively inhibit the proliferation of colorectal cancer cells carrying TP53 defects or belonging to the consensus molecular subtype CMS4. NCT02 has the potential to inhibit tumor growth in in vitro and in vivo models.
    NCT02
  • HY-126456
    (S,R,S)-AHPC-propargyl 2098799-78-9 99.46%
    (S,R,S)-AHPC-propargyl (VH032-propargyl) is a VHL ligand which is used in “click reaction” for PROTACs. (S,R,S)-AHPC-propargyl is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    (S,R,S)-AHPC-propargyl
  • HY-W037848
    Adamantan-1-ylmethanamine 17768-41-1 99.42%
    Adamantan-1-ylmethanamine (1-Aminomethyladamantane) is a Hyt hydrophobic group. Adamantan-1-ylmethanamine can be used in the synthesis of ZX782 (HY-161972).
    Adamantan-1-ylmethanamine
  • HY-133144
    Lenalidomide-OH 1416990-08-3 99.48%
    Lenalidomide-OH is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein. Lenalidomide-OH can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC BTK degrader SJF620 (HY-133137).
    Lenalidomide-OH
  • 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-125292
    NV03 2448341-58-8 99.77%
    NV03 is a potent and selective antagonist of Ubiquitin-like with PHD and RING finger domains 1 (UHRF1)-H3K9me3 interaction by binding to UHRF1 tandem tudor domain, with a Kd of 2.4 μM. NV03 is also a ligand for E3 ligase. NV03 can be studied in anticancer research.
    NV03
  • HY-175452
    MRT-3486 99.62%
    MRT-3486 is a molecular glue degrader.MRT-3486 induces ternary complex formation between CRBN and predicted β-hairpin G-loop proteins.MRT-3486 is selected from an internal compound library for proximity-ligation experiments.
    MRT-3486
  • HY-W076696
    3-(4-Hydroxy-1-oxoisoindolin-2-yl)piperidine-2,6-dione 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.
    3-(4-Hydroxy-1-oxoisoindolin-2-yl)piperidine-2,6-dione
  • HY-W069604
    Thalidomide-5-Br 26166-92-7 98.92%
    Thalidomide-5-Br (compound 4) is a compound with a bromodomain. Thalidomide-5-Br can be used in the research of inflammation, tumor and neurology.
    Thalidomide-5-Br
  • HY-149935
    OICR-8268 3000549-26-5 99.23%
    OICR-8268 is a reversible DCAF1 ligand that binds to the DCAF1 WDR domain with a Kd of 38 nM. OICR-8268 can enable the development of DCAF1-based PROTACs.
    OICR-8268
  • HY-14658R
    Thalidomide (Standard) 50-35-1
    Thalidomide (Standard) is the analytical standard of Thalidomide. This product is intended for research and analytical applications. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ∼250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide can work as molecular glue to potentiate substrate.
    Thalidomide (Standard)
  • HY-W1004786
    CRBN ligand-13 3050687-70-9
    CRBN ligand-13 is a CRBN-type E3 ubiquitin ligase ligand that can be used to prepare PROTAC.
    CRBN ligand-13
  • HY-W023573
    5-Aminothalidomide 191732-76-0 99.69%
    5-Aminothalidomide is an E3 ligase ligand used in PROTAC technology. 5-Aminothalidomide can be used to synthesize various PROTACs, such as the PROTAC BRD9 Degrader-7 (HY-155361).
    5-Aminothalidomide
  • 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-W013021
    Norbornene 498-66-8 99.95%
    Norbornene is a cycloolefin and building block for synthesis of porous organic polymeric materials via metathesis, addition, and CANAL polymerization. Norbornene can also be used as an E3 ligase ligand for the synthesis of PROTAC, such as PROTAC HyTTD Degrader-1 (HY-181895).
    Norbornene
  • HY-42419
    (S,R,S)-AHPC-Me-NHBoc 1997302-16-5 98.26%
    (S,R,S)-AHPC-Me-NHBoc is an E3 ubiquitin ligase VHL ligand used to recruit the VHL protein. (S,R,S)-AHPC-Me-NHBoc can be linked to a target protein ligand via a linker to form a PROTAC.
    (S,R,S)-AHPC-Me-NHBoc
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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