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-123109A
    (S,S,S)-AHPC-Boc 1797406-74-6
    (S,S,S)-AHPC-Boc is the isomer of (S,R,S)-AHPC-Boc (HY-123109), and can be used as an experimental control. (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,S,S)-AHPC-Boc
  • HY-131385
    KB02-COOH 2375196-30-6 99.39%
    KB02-COOH is a fragment of synthesis of ubiquitin E3 ligase ligand KB02. KB02 can be used in the synthesis of PROTAC, such as KB02-JQ1 (HY-129917) and KB02-SLF (HY-129610).
    KB02-COOH
  • 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-W761299
    PD 4'-oxyacetic acid 2633633-12-0 99.69%
    PD 4'-oxyacetic acid is a carboxylic acid-functionalized cereblon ligand that can be used for PROTAC Degrader development.
    PD 4'-oxyacetic acid
  • HY-114406
    TD-106 2250288-69-6 99.81%
    TD-106 is a cereblon (CRBN) modulator, which can be used for targeted protein degradation. BRD4 PROTACs with TD-106 induce BRD4 degradation.
    TD-106
  • HY-123215
    CC-17369 1547162-46-8 98.68%
    CC-17369 (7-Hydroxy pomalidomide) is a metabolite of Pomalidomide. CC-17369 is the Pomalidomide -based cereblon (CRBN) ligand used in the recruitment of CRBN protein. CC-17369 can be connected to the ligand for protein by a linker to form PROTAC.
    CC-17369
  • HY-138678
    (R,S,S)-VH032 2230826-33-0 98.99%
    (R,S,S)-VH032 is Ligand for E3 Ligase used in the synthesis of PROTACs. VH032 is a VHL ligand and VHL/HIF-1α interaction inhibitor that recruits von Hippel-Lindau (VHL) proteins. (R,S,S)-VH032 synthesizes the tau-targeting small molecule PROTAC C004019 (HY-138669).
    (R,S,S)-VH032
  • HY-123324
    Pomalidomide-5-OH 1547162-41-3 99.46%
    Pomalidomide-5-OH (5-hydroxy pomalidomide) is the Pomalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide-5-OH can be connected to the ligand for protein by a linker to form PROTAC.
    Pomalidomide-5-OH
  • HY-130845A
    AR antagonist 1 hydrochloride 1818885-55-0 99.53%
    AR antagonist 1 (compound 29) hydrochloride is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020).
    AR antagonist 1 hydrochloride
  • HY-W241635
    Thalidomide acid 1547163-38-1 ≥98.0%
    Thalidomide acid is a Thalidomide analog that can be useful in PROTAC research.
    Thalidomide acid
  • HY-W243404
    3-(6-Bromo-1-oxoisoindolin-2-yl)piperidine-2,6-dione 2304513-76-4 99.95%
    3-(6-Bromo-1-oxoisoindolin-2-yl)piperidine-2,6-dione is a Lenalidomide analog that can be useful in PROTAC research.
    3-(6-Bromo-1-oxoisoindolin-2-yl)piperidine-2,6-dione
  • HY-W249500
    2-Methoxyphenyl dihydrouracil 2377643-33-7
    2-Methoxyphenyl dihydrouracil (Compound 13) is a CRBN ligand, and can be used for synthesis of PROTACs.
    2-Methoxyphenyl dihydrouracil
  • 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-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-157566
    Lenalidomide 5'-piperazine-4-methylpiperidine hydrochloride 2520105-60-4
    Lenalidomide 5'-piperazine-4-methylpiperidine hydrochloride is a functionalized cerebellar ligand for PROTAC development, combining E3 ligand and terminal piperidine for subsequent chemical reactions. A protein degradant with a rigid connector is generated.
    Lenalidomide 5'-piperazine-4-methylpiperidine hydrochloride
  • HY-W259932
    Lenalidomide 5'-piperazine 2222120-31-0 99.92%
    Lenalidomide 5'-piperazine is a functionalized cerebellar ligand for PROTAC development that binds an E3 ligand to terminal piperazine for subsequent chemical reactions to produce a protein deactivator with a rigid linker.
    Lenalidomide 5'-piperazine
  • HY-138040
    CRBN modulator-1 2407829-65-4 98.00%
    CRBN modulator-1, a Thalidomide analog and a CRBN modulator extracted from WO2020006262A1, compound 10, has an IC50 of 3.5 μM and a Ki of 0.98 μM.
    CRBN modulator-1
  • HY-W076313
    2-(2,6-Dioxopiperidin-3-yl)-4-iodoisoindoline-1,3-dione 959150-64-2 99.88%
    2-(2,6-Dioxopiperidin-3-yl)-4-iodoisoindoline-1,3-dione is a derivative of Thalidomide with an iodine atom on the benzyl ring
    2-(2,6-Dioxopiperidin-3-yl)-4-iodoisoindoline-1,3-dione
  • HY-W898989
    3-(4-Bromo-2-chlorophenyl)piperidine-2,6-dione 2923549-60-2 98.92%
    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-47851
    VH 101, thiol 2358775-81-0 98.66%
    VH 101, thiol (compound 20) is a VHL ligand for the synthesis of PROTACs.
    VH 101, thiol
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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