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-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
  • HY-161197
    Thalidomide-2,6-diazaspiro[3.4]octane-C-piperidine-C2-O-C2-OH
    Thalidomide-2,6-diazaspiro[3.4]octane-C-piperidine-C2-O-C2-OH is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-2,6-diazaspiro[3.4]octane-C-piperidine-C2-O-C2-OH can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Thalidomide-2,6-diazaspiro[3.4]octane-C-piperidine-C2-O-C2-OH
  • HY-W584525
    VH032-NH-CO-CH2-NHBoc 2010986-19-1
    VH032-NH-CO-CH2-NHBoc is a Boc-modified VH032 (HY-120217) that acts as a ligand for VHL to recruit von Hippel-Lindau (VHL) proteins. VH032-NH-CO-CH2-NHBoc will remove the Boc protection under acidic conditions, and connect with the target protein ligand through a linker to form a PROTAC molecule, which is a key intermediate for the synthesis of PROTAC based on VHL ligand.
    VH032-NH-CO-CH2-NHBoc
  • HY-179733
    CRBN ligand-191 1519514-63-6
    CRBN ligand-191 is an E3 ligand that can be used for the synthesis of PROTACs, such as PROTAC ALK degrader-4 (HY-179732).
    CRBN ligand-191
  • HY-172948
    VHL Ligand 36 2250056-48-3
    VHL Ligand 36 is a von Hippel-Lindau (VHL) ligand. VHL Ligand 36 can be used to synthesize SD-2301 (HY-172946).
    VHL Ligand 36
  • HY-203082
    4-[(1E)-2-Nitroethenyl]benzoic acid 821797-33-5
    4-[(1E)-2-Nitroethenyl]benzoic acid is an E3 ligase ligand. 4-[(1E)-2-Nitroethenyl]benzoic acid can be used for synthesis of PROTAC BRD4 Degrader-38 (HY-175240).
    4-[(1E)-2-Nitroethenyl]benzoic acid
  • HY-W947273
    CRBN ligand-898 2766178-72-5
    CRBN ligand-898 is a CRBN ligand with a Kd of 216 nM. CRBN ligand-898 binds to CRBN, and when incorporated into proteolysis targeting chimeras (PROTACs), mediates degradation of intended target proteins. CRBN ligand-898 does not induce degradation of IMiD-associated neosubstrates Ikaros (IKZF1) and Aiolos (IKZF3). CRBN ligand-898 can be used to synthesize PROTACs.
    CRBN ligand-898
  • HY-163237
    Thalidomide-piperidine-O-azetidineethanol
    Thalidomide-piperidine-O-azetidineethanol is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-piperidine-O-azetidineethanol can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Thalidomide-piperidine-O-azetidineethanol
  • HY-170126S
    9-Amino-1,2,3,4-tetrahydroacridin-1-ol-d3 Maleate 1219806-48-0
    9-Amino-1,2,3,4-tetrahydroacridin-1-ol-d3 Maleate is the deuterium labeled CRBN ligand-74 (HY-170126). CRBN ligand-74 is a CRBN-type E3 ubiquitin ligase ligand that can be used to prepare PROTAC.
    9-Amino-1,2,3,4-tetrahydroacridin-1-ol-d<sub>3</sub> Maleate
  • HY-W890189
    E3 ligase Ligand 54 2413038-90-9
    E3 ligase Ligand 54 is the ligand for E3 ligase Cereblon and can be used for synthesis of PROTAC Degrader SJ44236 (HY-170900).
    E3 ligase Ligand 54
  • HY-157558
    KDRLKZ-1
    KDRLKZ-1 is a KLHDC2 ligand (Kd = 0.36 μM), with IC50s of 0.21 μM and 0.31 μM in alphaLISA and time-resolved fluorescence resonance energy transfer (TR-FRET) displacement assays.
    KDRLKZ-1
  • HY-180973
    CRBN ligand-893
    CRBN ligand-893 (Compound 4) is a CRBN ligand with a Kd of 0.2 μM. CRBN ligand-893 forms a PROTAC molecule by connecting to the target protein ligand via a linker. CRBN ligand-893 can also be used in molecular glue research.
    CRBN ligand-893
  • HY-183011
    CRBN ligand-901 2953426-96-3
    CRBN ligand-901 (5d in Scheme 2) is a ligand for Cereblon (CRBN). CRBN ligand-901 can be linked to target protein ligands (e.g., VP1 ligand-1) via a linker to form PROTAC molecules (e.g., Jun15702 (HY-182924)).
    CRBN ligand-901
  • HY-163210
    Pomalidomide 5'-fluoro-6'-piperazine-4-methylpiperidine hydrochloride 2758431-94-4
    Pomalidomide 5'-fluoro-6'-piperazine-4-methylpiperidine hydrochloride (ZJT1) is an E3 ubiquitin ligase cereblon based on Pomalidomide (HY-10984) (CRBN) ligand for recruitment of cereblon protein. Pomalidomide 5'-fluoro-6'-piperazine-4-methylpiperidine hydrochloride can be linked to protein ligand by linker to form PROTAC.
    Pomalidomide 5'-fluoro-6'-piperazine-4-methylpiperidine hydrochloride
  • HY-W288798
    DCAF11 ligand 2 24044-52-8
    DCAF11 ligand 2 is an E3 ligase ligand that can be used in the recruitment of DCAF11. DCAF11 ligand 2 can be connected to the BRD4 ligand (HY-78695) by a linker to synthesis of PROTAC BRD4 degrader LGF308 (HY-181756).
    DCAF11 ligand 2
  • HY-N0215S16
    L-Phenylalanine-13C-1 136056-01-4
    L-Phenylalanine-13C-1 ((S)-2-Amino-3-phenylpropionic acid-13C-1) is the 13C-labeled L-Phenylalanine (HY-N0215). L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca2+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (Kb of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals.
    L-Phenylalanine-<sup>13</sup>C-1
  • HY-183818
    CRBN ligand-903
    CRBN ligand-903 is a CRBN-binding ligand as well as a ligand for E3 ubiquitin ligase (Ligands for E3 Ligase). CRBN ligand-903 can be used to synthesize PROTAC CBP/P300 Degrader-4 (HY-183802).
    CRBN ligand-903
  • HY-181042
    CRBN ligand-895 2782024-56-8
    CRBN ligand-895 (Compound 14) is an E3 ubiquitin ligase ligand for cereblon (CRBN), which is used to recruit the cereblon protein. CRBN ligand-895 can be used for the synthesis of PROTACs, such as PROTAC HDAC8 Degrader-4 (HY-181024).
    CRBN ligand-895
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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