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 (298):

Cat. No. Product Name Effect Purity
  • 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-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-130737
    Pomalidomide 4'-alkylC5-acid 98.78%
    Pomalidomide 4'-alkylC5-acid (Example 3) is an E3 ligase ligand-linker conjugate containing a Pomalidomide (HY-10984) based cereblon (CRBN) ligand and a linker. Pomalidomide 4'-alkylC5-acid can be used in the synthesis of PROTAC[1].
  • HY-137531
    Pomalidomide-PEG1-C2-COOH 99.88%
    Pomalidomide-PEG1-C2-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 1-unit PEG linker used in PROTAC technology[1].
  • HY-112495
    VH032-PEG5-C6-Cl
    VH032-PEG5-C6-Cl (HaloPROTAC 2) is a conjugate of ligands for E3 and 21-atom-length linker. The connector of linker is Halogen group. VH032-PEG5-C6-Cl incorporates the VH032 based VHL ligand and 5-unit PEG linker. VH032-PEG5-C6-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays[1].
  • HY-148406
    (S,R,S)-AHPC-C10-NHBoc 98.32%
    (S,R,S)-AHPC-C10-NHBoc is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC (HY-125845) based VHL ligand and a linker used for BET-Targeted PROTAC[1].
  • HY-138786A
    Thalidomide-5-PEG3-NH2 hydrochloride
    Thalidomide-5-PEG3-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology[1].
  • HY-148671
    (S,R,S)-AHPC-amido-C7-acid 98.28%
    (S,R,S)-AHPC-amido-C7-acid incorporates a VHL ligand for the E3 ubiquitin ligase and a PROTAC linker. (S,R,S)-AHPC-amido-C5-acid can be used to design PROTACs[1].
  • 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
    (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-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].
  • HY-138771
    Thalidomide-NH-PEG3-COOH 98.33%
    Thalidomide-NH-PEG3-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology[1].
  • HY-128822
    cIAP1 Ligand-Linker Conjugates 13
    cIAP1 Ligand-Linker Conjugates 13 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 13 can be used to design SNIPERs[1].
  • HY-128813A
    cIAP1 Ligand-Linker Conjugates 15 hydrochloride
    cIAP1 Ligand-Linker Conjugates 15 hydrochloride incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 15 hydrochloride can be used to design SNIPERs[1].
  • HY-136186
    (S,R,S)-AHPC-C7-amine
    (S,R,S)-AHPC-C7-amine (VH032-C7-amine) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for estrogen-related receptor α (ERRα) PROTAC degrader[1].
  • HY-132208
    Pomalidomide 4'-PEG2-azide 99.24%
    Pomalidomide 4'-PEG2-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology[1].
  • HY-141012
    Thalidomide-O-PEG4-NHS ester 98.23%
    Thalidomide-O-PEG4-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].