1. Signaling Pathways
  2. PROTAC
  3. Ligands for E3 Ligase

Ligands for E3 Ligase

E3 ligase-recruiting Moiety

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).

Cat. No. 상품명 CAS No. Purity 화학구조
  • HY-43983
    CRBN ligand-798 1448189-90-9
    CRBN ligand-798 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. CRBN ligand-798 can be linked to a target protein ligand via a linker to form a PROTAC.
    CRBN ligand-798
  • 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-157566
    Lenalidomide 5'-piperazine-4-methylpiperidine hydrochloride 2520105-60-4 98.57%
    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-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-138881
    Lenalidomide-6-F 2468780-87-0 99.63%
    Lenalidomide-6-F is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-6-F can be connected to the ligand for protein by a linker to form PROTAC.
    Lenalidomide-6-F
  • HY-W457960
    2-(2,6-Dioxopiperidin-3-yl)-5-ethynylisoindoline-1,3-dione 2154356-63-3 98.66%
    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-W251343
    Desamino lenalidomide-6-OH 1416990-09-4 99.36%
    Desamino lenalidomide-6-OH is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. Desamino lenalidomide-6-OH can be linked to a target protein ligand via a linker to form a PROTAC.
    Desamino lenalidomide-6-OH
  • HY-W244728
    Desamino lenalidomide-pinacolborane 2291363-98-7 ≥98.0%
    Desamino lenalidomide-pinacolborane is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. Desamino lenalidomide-pinacolborane can be linked to a target protein ligand via a linker to form a PROTAC.
    Desamino lenalidomide-pinacolborane
  • HY-W598447
    CRBN ligand-734 2654830-24-5 ≥98.0%
    CRBN ligand-734 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. CRBN ligand-734 can be linked to a target protein ligand via a linker to form a PROTAC.
    CRBN ligand-734
  • 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-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-150803
    VHL Ligand 14 2010986-87-3 99.93%
    VHL Ligand 14 (Compound 11) is a VHL ligand for design of PROTAC estrogen receptor α (ERα) degraders, with a binding affinity IC50 of 196 nM.
    VHL Ligand 14
  • HY-175686
    E3 ligase Ligand 67 98.69%
    E3 ligase Ligand 67 (Compound 5) is a STUB1/CHIP ligand with a Kd of 8.9  μM for CHIP in fluorescence polarization assay. E3 ligase Ligand 67 is an E3 ligase ligand that can be used for synthesis of PROTACs.
    E3 ligase Ligand 67
  • HY-133045
    VHL Ligand 8 2701565-76-4 98.04%
    VHL Ligand 8 is a VHL ligand. VHL Ligand 8 can be used to synthesize ARD-266 (HY-133020), a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM.
    VHL Ligand 8
  • HY-148880
    VHLL-BCN 2874203-49-1
    VHLL-BCN is a ligand targeting the VHL E3 ligase, which can be used for the synthesis of PROTAC molecules. As a key component of the copper-free SPAAC-based rapid synthesis platform for transcription factor PROTACs, VHLL-BCN is applicable to cancer-related research.
    VHLL-BCN
  • 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-176036
    MS1262 3070323-06-4 98.61%
    MS1262 is a ligand for the E3 enzyme SPOP substrate GLP and can recruit SPOP. MS1262 can be used to synthesize MS479 (HY-176035).
    MS1262
  • 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-W460201
    CRBN ligand-660 2154343-28-7 98.31%
    CRBN ligand-660 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. CRBN ligand-660 can be linked to a target protein ligand via a linker to form a PROTAC.
    CRBN ligand-660
  • HY-W458077
    Desamino lenalidomide-7-OH 1416990-10-7 99.11%
    Desamino lenalidomide-7-OH is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. Desamino lenalidomide-7-OH can be linked to a target protein ligand via a linker to form a PROTAC.
    Desamino lenalidomide-7-OH
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