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-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-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-W440247
    CRBN ligand-109 2758533-77-4 ≥98.0%
    CRBN ligand-109 is a CRBN-type E3 ubiquitin ligase ligand that can be used to prepare PROTAC.
    CRBN ligand-109
  • 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
    (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-144985
    E3 ligase Ligand 23 444287-56-3 99.71%
    E3 ligase Ligand 23 (compound 17-6) is a cereblon binder for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway.
    E3 ligase Ligand 23
  • HY-W039233
    Lenalidomide-F 2359705-88-5 99.89%
    Lenalidomide-F is a E3 ligase ligand for LWY713. LWY713 is a PROTAC-class FLT3 degrader (DC50 = 0.64 nM), which selectively induces FLT3 degradation via cereblon and proteasome-dependent pathways.
    Lenalidomide-F
  • HY-W243404
    3-(6-Bromo-1-oxoisoindolin-2-yl)piperidine-2,6-dione 2304513-76-4 99.85%
    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-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
  • HY-136164
    VH032-OH 2244684-42-0 99.43%
    VH032-OH is the VH032-based VHL ligand. VH032-OH can be connected to the ligand for protein by a linker to form PROTACs.
    VH032-OH
  • HY-153215
    MEL24 642072-48-8 ≥98.0%
    MEL24 is an Mdm2 E3 ligase inhibitor that reduces cell survival and increases sensitivity to DNA damaging agents in a p53-dependent manner for in vitro antitumor studies.
    MEL24
  • 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-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-W342590
    CRBN ligand-9 55003-81-1 ≥98.0%
    CRBN ligand-9 (Compound 4d) is a CRBN ligand (Ki: 8.9 μM). CRBN ligand-9 can be used for synthesis of PROTACs.
    CRBN ligand-9
  • HY-10984S1
    Pomalidomide-d3 2093128-28-8 ≥99.0%
    Pomalidomide-d3 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[1][2].
    Pomalidomide-d<sub>3</sub>
  • HY-151227
    VL285 Phenol 1448188-69-9 98.56%
    VL285 Phenol is a phenol-based VL285 analog. VL285 is an E3 ubiquitin ligase VHL ligand and can be used in the synthesis of HaloPROTAC3, degrading HaloTag7 fusion protein (IC50=0.34 μM).
    VL285 Phenol
  • HY-149935
    OICR-8268 3000549-26-5
    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-W076313
    2-(2,6-Dioxopiperidin-3-yl)-4-iodoisoindoline-1,3-dione 959150-64-2
    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-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)
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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