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. 상품명 CAS No. Purity 화학구조
  • HY-W883787
    Hydrouracil-4-fluorobenzoate 2377643-38-2
    Hydrouracil-4-fluorobenzoate is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. Hydrouracil-4-fluorobenzoate can be linked to a target protein ligand via a linker to form a PROTAC.
    Hydrouracil-4-fluorobenzoate
  • HY-W883327
    CRBN ligand-430 2925071-04-9
    CRBN ligand-430 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. CRBN ligand-430 can be linked to a target protein ligand via a linker to form a PROTAC.
    CRBN ligand-430
  • HY-W883326
    CRBN ligand-902 2913408-82-7
    CRBN ligand-902 is a CRBN E3 ligase ligand that can be used for synthesis of PROTAC CDK2/4 Degrader-1 (HY-179688).
    CRBN ligand-902
  • HY-W586333
    Desamino lenalidomide-5-C-COOH 2287262-43-3
    Desamino lenalidomide-5-C-COOH is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. Desamino lenalidomide-5-C-COOH can be linked to a target protein ligand via a linker to form a PROTAC.
    Desamino lenalidomide-5-C-COOH
  • HY-A0003A
    Lenalidomide hydrochloride 1243329-97-6
    Lenalidomide hydrochloride (CC-5013 hydrochloride), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hydrochloride is an orally active immunomodulator. Lenalidomide hydrochloride (CC-5013 hydrochloride) 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 hydrochloride (CC-5013 hydrochloride) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells.
    Lenalidomide hydrochloride
  • HY-110402
    (S,R,S)-AHPC TFA 1631137-51-3
    (S,R,S)-AHPC (VH032-NH2) TFA is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC TFA 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 TFA
  • HY-D3392
    Thalidomide-cyanine 5
    Thalidomide-cyanine 5 is a fluorescent probe prepared by conjugating the CRBN binder Thalidomide (HY-14658) with the near-infrared fluorescent dye Cy5. Thalidomide-cyanine 5 binds to DDB1-CRBN protein complex with a Kd of 121.6 nM. Thalidomide-cyanine 5 binds to CRBN to form a binary complex, and is mainly used for the visual tracking research of degradants such as PROTAC (Ex/Em = 650/665 nm).
    Thalidomide-cyanine 5
  • HY-181791
    VHL Ligand 39 2876809-75-3
    VHL Ligand 39 is a conjugate of an E3 ligase ligand, serving as a key intermediate in the synthesis of complete PROTAC molecules.
    VHL Ligand 39
  • HY-D2259
    PFI-7 2910938-58-6
    PFI-7 is a probe, which binds to human GID4 (KD is 79 nM), and antagonizes the binding of Pro/N-degrons. PFI-7 can be utilized in C-terminal to LisH (CTLH) complex research and development of targeted protein degradation.
    PFI-7
  • HY-W597583
    2-(2,6-Dioxopiperidin-3-yl)phthalimidine NMe 26581-83-9
    2-(2,6-Dioxopiperidin-3-yl)phthalimidine NMe is an E3 ligase ligand of SIAIS630121-NC (HY-159016). 2-(2,6-Dioxopiperidin-3-yl)phthalimidine NMe contains an extra methyl group on the glutarimide moiety of thalidomide, which is known to abrogate its ability to bind the E3 ligase CRBN. SIAIS630121-NC is a negative control for NAMPT degrader SIAIS630121.
    2-(2,6-Dioxopiperidin-3-yl)phthalimidine NMe
  • HY-181530
    IAP ligand 6
    IAP ligand 6 (A250) is an IAP ligand that can be used for the synthesis of PROTACs, such as PROTAC TEAD1/IAP degrader-1 (HY-181534).
    IAP ligand 6
  • HY-W077589A
    Lenalidomide-5-aminomethyl 1010100-28-3
    Lenalidomide-5-aminomethyl is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-5-aminomethyl can be connected to the ligand for protein by a linker to form PROTAC.
    Lenalidomide-5-aminomethyl
  • HY-161467
    Aster-A Ligand-3 2375541-28-7
    Aster-A Ligand-3 is a target protein ligand and can be used to synthesize PROTAC Aster-A degrader (HY-D2336).
    Aster-A Ligand-3
  • HY-180280
    KLHDC2 ligand 3
    KLHDC2 ligand 3 is an E3 ligase ligand. KLHDC2 ligand 3 can be used for the synthesis of PROTAC CDK6 Degrader 1 (HY-180277).
    KLHDC2 ligand 3
  • HY-161639
    E3 ligase Ligand 26 2911613-35-7
    E3 ligase Ligand 26 (part of Compd 10) is a ligand for E3 ligase, used for the synthesis of PROTAC SOS1 degrader (HY-161636).
    E3 ligase Ligand 26
  • HY-128806
    E3 ligase Ligand 9 87304-15-2
    E3 ligase Ligand 9 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 9 can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
    E3 ligase Ligand 9
  • HY-157560
    KDRLKZ-3
    KDRLKZ-3 is a selective E3 ligase. KDRLKZ-3 is a ligand for KLHDC2 with a IC50 value of 4.1 μM in the alphaLISA experiment.
    KDRLKZ-3
  • HY-170353
    E3 ligase Ligand 46 3033591-48-6
    E3 ligase Ligand 46 is a ligand for E3 ligase, used for the synthesis of PROTAC SMARCA2/4 degrader-36 (HY-170347).
    E3 ligase Ligand 46
  • HY-W1003189
    E3 ligase Ligand 42 2753651-18-0
    E3 ligase Ligand 42 is an E3 ubiquitin ligase ligand. E3 ligase Ligand 42 can be connected to the target protein ligand through a linker and can be used to synthesize PROTAC AR Degrader-6 (HY-156751). PROTAC can induce ubiquitination degradation of cancer-promoting proteins.
    E3 ligase Ligand 42
  • HY-176386
    E3 ligase Ligand 68 1466558-44-0
    E3 ligase Ligand 68 is an E3 ligase ligand that can be used in the synthesis of PROTACs, such as PROTAC ER Degrader-3 (HY-128527).
    E3 ligase Ligand 68
Cat. No. 상품명 / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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