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 (340):

Cat. No. Product Name Effect Purity
  • HY-103599
    (S,R,S)-AHPC-PEG2-N3 99.74%
    (S,R,S)-AHPC-PEG2-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-PEG2-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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
  • 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-103601
    (S,R,S)-AHPC-PEG4-N3 99.73%
    (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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
  • HY-130271
    (S,R,S)-AHPC-PEG5-COOH 99.88%
    (S,R,S)-AHPC-PEG5-COOH (VH032-PEG5-COOH) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 5-unit PEG linker used in PROTAC technology[1].
  • 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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
  • HY-157752
    E3 Ligase Ligand-linker Conjugate 101
    E3 Ligase Ligand-linker Conjugate 101 is a conjugate of E3 ligase ligand and linker, consisting of (S,R,S)-AHPC (HY-125845) and the corresponding Linker. (S,R,S)-AHPC is a VH032-based von Hippel-Lindau (VHL) ligand that recruits VHL proteins. E3 Ligase Ligand-linker Conjugate 101 can be used as a key intermediate for the synthesis of complete PROTAC molecules.
  • HY-157749
    Thalidomide-piperazine-(S)-CH2-pyrrolidine-C2-O-CH2-COO-C(CH3)3
    Thalidomide-piperazine-(S)-CH2-Pyrrolidine-C2-O-CH2-COO-C (CH3)3 is a synthetic E3 ligase ligand-Linker conjugate. Thalidomide-piperazine-(S)-Ch2-Pyrrolidine-C2-O-CH2-COO-C(CH3)3 includes Thalidomide-based cereblon ligands and linkers. Thalidomide-piperazine-(S)-CH2-Pyrrolidine-C2-O-CH2-COO-C(CH3)3 can be used to synthesize PROTAC BET[1].
  • HY-145449A
    CC-885-CH2-PEG1-NH-CH3 TFA 99.28%
    CC-885-CH2-PEG1-NH-CH3 TFA is a new degrader that can be used to synthesize antibody-based novel degrader conjugated active molecules (AnDC)[1][2].
  • 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-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-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-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].