2. PROTAC
  3. E3 Ligase Ligand-Linker Conjugates

E3 Ligase Ligand-Linker Conjugates

E3 Ligase Ligand-Linker Conjugate, which is one part of Proteolysis Targeting Chimeric Molecules (PROTACs), incorporates a ligand for the E3 ubiquitin ligase and a linker. After linked to the ligand for target protein (such as JQ1 for BRD4 protein, Molibresib for BET protein), those conjugates can be used for constituting PROTACs that targetprotein for ubiquitination and degradation. Currently, several PROTACs have been found to show good biological activity by specifically targeting BET, estrogen receptor (ER), androgen receptor, etc. MedChemExpress (MCE) offers a wide range of high quality E3 Ligase Ligand-Linker Conjugates including von Hippel-Lindau (VHL) ligands, MDM2 ligands, Cereblon (CRBN) ligands and cIAP1 ligands conjugating with different linkers (PEGs, Alkyl-Chain, Alkyl/ether, etc.). It’s convenient and time-saving for designing and synthesizinga wide variety of novel PROTACs (ARV-825, dBET1,MT-802, etc.), which can expand the application of PROTACs in the treatment of cancer, autoimmunity, inflammation and other diseases.

E3 Ligase Ligand-Linker Conjugates Related Products (714):

Cat. No. Product Name Effect Purity
  • HY-111997
    VH285-PEG4-C4-Cl
    VH285-PEG4-C4-Cl (HaloPROTAC 3) is a conjugate of ligands for E3 and 16-atom-length linker. The connector of linker is Halogen group. VH285-PEG4-C4-Cl incorporates the VH285 based VHL ligand and an alkyl/ether-based linker. VH285-PEG4-C4-Cl is a highly potent and efficacious degrader of GFP-HaloTag7 with a DC50 of 19 nM. VH285-PEG4-C4-Cl is able to induce 90 % degradation of GFP-Halotag at 625 nM. VH285-PEG4-C4-Cl binds to VHL with an IC50 of 0.54 μM[1].
  • HY-145448
    MC-VC-PABC-amide-PEG1-CH2-CC-885 99.93%
    MC-VC-PABC-amide-PEG1-CH2-CC-885 (compound I-1) is a neoDegrader-Linker conjugate, consists of the GSPT1 degrader/molecular glue CC-885 (HY-101488) and a linker. MC-VC-PABC-amide-PEG1-CH2-CC-885 can be conjugated to the antibody DAR3.7 that specifically targets CD56 to synthesize Antibody-Drug Conjugates (ADCs)[1].
  • HY-103601
    (S,R,S)-AHPC-PEG4-N3 99.93%
    (S,R,S)-AHPC-PEG4-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-PEG4-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
  • HY-103598
    (S,R,S)-AHPC-PEG3-N3 99.67%
    (S,R,S)-AHPC-PEG3-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 3-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-PEG3-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
  • HY-145449
    CC-885-CH2-PEG1-NH-CH3 99.22%
    CC-885-CH2-PEG1-NH-CH3 is a neoDegrader that can be used in the synthesis of Antibody neoDegrader Conjugate (AnDC)[1][2].
  • HY-172625
    VH 101-amide-piperidine-Pip-alkyne
    VH 101-amide-piperidine-Pip-alkyne is an E3 Ligase Ligand-Linker Conjugates that can be used to synthesize PROTAC degrader. The linker part of VH 101-amide-piperidine-Pip-alkyne is tert-Butyl 4-ethynyl-[1,4'-bipiperidine]-1'-carboxylate (HY-W442074), and the VHL-type E3 ubiquitinase ligand is VH 101, acid (HY-47070)[1].
  • HY-173628
    (R,S,S)-VH032-Me-N-Boc-7-aminoheptanoic acid
    (R,S,S)-VH032-Me-N-Boc-7-aminoheptanoic acid is a E3 Ligase Ligand-Linker Conjugate, consisting of N-Boc-7-aminoheptanoic acid (HY-W012001) and the corresponding Linker. (R,S,S)-VH032-Me-N-Boc-7-aminoheptanoic acid can be used for the synthesis of dTAGV-1-NEG (HY-145514A)[1].
  • HY-173628A
    (S,R,S)-AHPC-Me-N-Boc-7-aminoheptanoic acid
    (S,R,S)-AHPC-Me-N-Boc-7-aminoheptanoic acid is a conjugate of an E3 ligase ligand and a linker, which can be used for the synthesis of PROTAC dTAGV-1 TFA (HY-145514)[1].
  • HY-161130
    Lenalidomide 4'-PEG3-amine dihydrochloride
    Lenalidomide 4'-PEG3-amine dihydrochloride is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide 4'-PEG3-amine dihydrochloride can be connected to the ligand for protein by a linker to form PROTAC[1].
  • HY-W584518
    Thalidomide-5-O-CH2-COOH
    Thalidomide-5-O-CH2-COOH is an E3 Ligase Ligand-Linker Conjugate consisting of Thalidomide (HY-14658) and NH-PEG3-NH-Boc. Thalidomide-5-O-CH2-COOH acts as a ligand for Cereblon to recruit CRBN protein. Thalidomide-5-O-CH2-COOH is a key intermediate in the synthesis of PROTAC molecules designed based on CRBN.
  • HY-W800760
    (S,R,S)-AHPC-PEG6-Tos
    (S, R, S)-AHPC-PEG6-Tos is a combination of a von Hippel-Lindau (VHL)-recruiting ligand and PEGylated crosslinker with a tosyl group. The tosyl group is a good leaving group for nucleophilic substitution reactions. (S, R, S)-AHPC-PEG2-Tos is useful for synthesis of PROTAC compounds and molecules for targeted protein degradation.
  • HY-122725B
    Lenalidomide-C5-NH2 hydrochloride 98.44%
    Lenalidomide-C5-NH2 hydrochloride is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C5-NH2 can be connected to the ligand for protein by a linker to form PROTACs, such as MDM2 PROTAC degrader[1][2].
  • HY-157756
    E3 Ligase Ligand-linker Conjugate 104
    E3 Ligase Ligand-linker Conjugate 104 is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. E3 Ligase Ligand-linker Conjugate 104 can serve as Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
  • HY-130642
    (S,R,S)-AHPC-Me-C10-Br
    (S,R,S)-AHPC-Me-C10-Br is a synthesized E3 ligase ligand-linker conjugate. (S,R,S)-AHPC-Me-C10-Br incorporates a VHL E3 ligase linker and MS432 based on the MEK1/2 inhibitor PD0325901[1].
  • HY-136006B
    (S,R,S)-AHPC-C6-NH2 98.03%
    (S,R,S)-AHPC-C6-NH2 (VH032-C6-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in?PROTAC?technology[1].
  • HY-148362
    Pomalidomide-C6-O-C5-O-C4-COOH 98.55%
    Pomalidomide-C6-O-C5-O-C4-COOH is a E3 ligase ligand-linker conjugate comprising a Pomalidomide (HY-10984)-based cereblon ligand and linker. Pomalidomide-C6-O-C5-O-C4-COOH can be used for the synthesis of PROTACs[1].
  • HY-133816A
    Pomalidomide-amino-PEG5-NH2
    Pomalidomide-amino-PEG5-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology[1].
  • HY-163167
    VH 032 amide-alkylC5-azide
    VH 032 amide-alkylC5-amine is a functionalized von-Hippel-Lindau protein ligand (VHL) for PROTAC research and development; incorporates an E3 ligase ligand plus an alkyl linker with terminal amine ready for conjugation to a target protein ligand[1].
  • HY-138792
    Glutarimide-Isoindolinone-NH-PEG2-COOH 98.51%
    Glutarimide-Isoindolinone-NH-PEG2-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates a cereblon ligand and a linker used in PROTAC technology[1].
  • HY-129941
    (S,R,S)-AHPC-C10-NH2
    (S,R,S)-AHPC-C10-NH2 (VH032-C10-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used for BET-Targeted PROTAC[1].