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-W460227
    Lenalidomide-4-Br-7-fluoro 2438239-34-8
    Lenalidomide-4-Br-7-fluoro is a derivative of Lenalidomide with a flouride and bromide groups on the benzyl ring.
    Lenalidomide-4-Br-7-fluoro
  • HY-160244
    Pomalidomide 5'-piperazine-4-methylpiperidine dihydrochloride 2758431-93-3 98.08%
    Pomalidomide 5'-piperazine-4-methylpiperidine dihydrochloride is the Pomalidomide (HY-10984)-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide 5'-piperazine-4-methylpiperidine dihydrochloride can be connected to the ligand for protein by a linker to form PROTAC.
    Pomalidomide 5'-piperazine-4-methylpiperidine dihydrochloride
  • HY-W586331
    Thalidomide-iodo 2509137-01-1 ≥98.0%
    Thalidomide-iodo is an iodinated E3 ligase activator. Thalidomide-iodo can be used for further derivitization by substitution of iodine.
    Thalidomide-iodo
  • HY-149561
    Thalidomide-5-O-C4-NH2 hydrochloride 2694727-93-8 99.98%
    Thalidomide-5-O-C4-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C4-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-O-C4-NH2 hydrochloride
  • HY-W586821
    Thalidomide-1-Me-5-NH2 1468761-60-5 ≥98.0%
    Thalidomide-1-Me-5-NH2 is an aminated Thalidomide analogue. E3 Ligase activators such as this may be used in the design of PROTAC molecules via derivatization at its amine.
    Thalidomide-1-Me-5-NH2
  • HY-W457960
    2-(2,6-Dioxopiperidin-3-yl)-5-ethynylisoindoline-1,3-dione 2154356-63-3
    2-(2,6-Dioxopiperidin-3-yl)-5-ethynylisoindoline-1,3-dione is a Thalidomide analog that can be useful in PROTAC research.
    2-(2,6-Dioxopiperidin-3-yl)-5-ethynylisoindoline-1,3-dione
  • HY-W898989
    3-(4-Bromo-2-chlorophenyl)piperidine-2,6-dione 2923549-60-2
    3-(4-Bromo-2-chlorophenyl)piperidine-2,6-dione is a CRBN-type E3 ubiquitin ligase ligand that can be used to prepare PROTAC.
    3-(4-Bromo-2-chlorophenyl)piperidine-2,6-dione
  • HY-130949B
    Thalidomide-4-O-C7-NH2 hydrochloride 99.80%
    Thalidomide-4-O-C7-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-4-O-C7-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-4-O-C7-NH2 hydrochloride
  • HY-14658B
    (R)-Thalidomide 2614-06-4 99.80%
    (R)-Thalidomide ((R)-(+)-Thalidomide) is the R-enantiomer of Thalidomide. (R)-Thalidomide has psychomotor stabilizing properties.
    (R)-Thalidomide
  • HY-W586329
    Thalidomide-4-carbaldehyde 2369068-46-0
    Thalidomide-4-carbaldehyde is a Thalidomide analogue with an aldehyde. Thalidomide recruiits E3 ligase for the ubiquitinylation and subsequent proteolysis of target proteins. The aldehyde is highly reactive towards amine nucleophiles through reductive amination among other reactions.
    Thalidomide-4-carbaldehyde
  • HY-W451211
    Thalidomide-5-carbaldehyde 1447701-63-4
    Thalidomide-5-carbaldehyde is a Thalidomide analogue with an aldehyde. Thalidomide recruiits E3 ligase for the ubiquitinylation and subsequent proteolysis of target proteins. The aldehyde is highly reactive towards amine nucleophiles through reductive amination among other reactions.
    Thalidomide-5-carbaldehyde
  • HY-W441376
    Thalidomide-1-Me,4-OH 2244568-06-5 ≥98.0%
    Thalidomide-1-Me,4-OH is a Thalidomide analogue featuring an alcohol. Thalidomide is a ligand for E3 ligase, which ubiquitinylates proteins, thus committing their fate to proteolytic destruction.
    Thalidomide-1-Me,4-OH
  • HY-149570
    Thalidomide-5-O-C13-NH2 hydrochloride 99.93%
    Thalidomide-5-O-C13-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C13-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-O-C13-NH2 hydrochloride
  • HY-W243405
    3-(7-Bromo-1-oxoisoindolin-2-yl)piperidine-2,6-dione 2229976-08-1 98.99%
    3-(7-Bromo-1-oxoisoindolin-2-yl)piperidine-2,6-dione is a Lenalidomide analog that can be useful in PROTAC research.
    3-(7-Bromo-1-oxoisoindolin-2-yl)piperidine-2,6-dione
  • HY-44249
    Thalidomide-CH2NH2 hydrochloride 444287-40-5
    Thalidomide-CH2NH2 hydrochloride is a Thalidomide analogue featuring a primary amine, which is a versatile group which may participate in many reactions.
    Thalidomide-CH2NH2 hydrochloride
  • 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-10984S2
    Pomalidomide-d4 1416575-78-4
    Pomalidomide-d4 is the deuterium labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors<
    Pomalidomide-d<sub>4</sub>
  • 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-161185
    Thalidomide-piperidine-O-azetidine-boc 2991611-55-1
    Thalidomide-piperidine-O-azetidine-boc is a conjugate of E3 ubiquitin ligase ligand-Linker, which can be used to synthesize complete PROTACs molecules.
    Thalidomide-piperidine-O-azetidine-boc
  • HY-157758
    (S)-Thalidomide-piperazine-pyrimidine-piperazine-C2-O-CH2-COO-C(CH3)3
    (S)-Thalidomide-piperazine-pyrimidine-piperazine-C2-O-CH2-COO-C(CH3)3 is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker . (S)-Thalidomide-piperazine-pyrimidine-piperazine-C2-O-CH2-COO-C(CH3)3 can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    (S)-Thalidomide-piperazine-pyrimidine-piperazine-C2-O-CH2-COO-C(CH3)3
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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