1. Signaling Pathways
  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.

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-103605
    (S,R,S)-AHPC-C6-PEG3-C4-Cl 1835705-55-9
    (S,R,S)-AHPC-C6-PEG3-C4-Cl (VH032-C6-PEG3-C4-Cl) is a conjugate of ligands for E3 and 20-atom-length linker. The connector of linker is Halogen group. (S,R,S)-AHPC-C6-PEG3-C4-Cl incorporates the (S,R,S)-AHPC based VHL ligand and an alkyl/ether-based linker. (S,R,S)-AHPC-C6-PEG3-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.
    (S,R,S)-AHPC-C6-PEG3-C4-Cl
  • HY-131647
    Pomalidomide 4'-PEG5-acid 2139348-63-1
    Pomalidomide 4'-PEG5-acid (Pomalidomide-PEG5-CO2H) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 5-unit PEG linker used in PROTAC technology.
    Pomalidomide 4'-PEG5-acid
  • HY-122725B
    Lenalidomide-C5-NH2 hydrochloride 2595367-27-2 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.
    Lenalidomide-C5-NH2 hydrochloride
  • HY-133799
    Pomalidomide-C7-COOH 2225940-51-0 98.07%
    Pomalidomide-C7-COOH is a synthesized E3 ligase cereblon ligand-linker conjugate. Pomalidomide-C7-COOH is an intermediate for the synthesis of PROTAC BCL-XL degraders.
    Pomalidomide-C7-COOH
  • HY-130737
    Pomalidomide 4'-alkylC5-acid 2225940-49-6 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.
    Pomalidomide 4'-alkylC5-acid
  • HY-130798
    (S,R,S)-AHPC-amido-C5-acid 2162120-87-6 99.58%
    (S,R,S)-AHPC-amido-C5-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 XY028-133 (HY-129180).
    (S,R,S)-AHPC-amido-C5-acid
  • HY-136237
    Thalidomide-NH-C5-NH2 hydrochloride 2375194-03-7 99.86%
    Thalidomide-NH-C5-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-NH-C5-NH2 hydrochloride
  • HY-103604
    (S,R,S)-AHPC-PEG4-NH2 hydrochloride 2064292-52-8 98.06%
    (S,R,S)-AHPC-PEG4-NH2 hydrochloride 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-NH2 hydrochloride
  • HY-133487B
    (S,R,S)-AHPC-C8-NH2 2341796-79-8
    (S,R,S)-AHPC-C8-NH2 (VH032-C8-NH2) is a synthesized?E3 ligase ligand-linker conjugate?that incorporates the VH032 based VHL ligand and a linker used for AKT PROTAC degrader. (S,R,S)-AHPC-C8-NH2 is XF038-164A, example 8, extracted from patent WO2019173516A1.
    (S,R,S)-AHPC-C8-NH2
  • HY-130683
    Lenalidomide-propargyl-C2-NH2 hydrochloride 2489242-23-9 98.04%
    Lenalidomide-propargyl-C2-NH2 hydrochloride incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase, and a linker. Lenalidomide-propargyl-C2-NH2 hydrochloride can be used to design the PROTAC MD-224 (HY-114312). Lenalidomide-propargyl-C2-NH2 (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Lenalidomide-propargyl-C2-NH2 hydrochloride
  • HY-130952
    Thalidomide-O-C8-COOH 2225148-51-4
    Thalidomide-O-C8-COOH is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-O-C8-COOH (Cereblon ligand 3) can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-O-C8-COOH
  • HY-122710A
    Thalidomide-O-amido-PEG4-C2-NH2 hydrochloride 2245697-85-0
    Thalidomide-O-amido-PEG4-C2-NH2 hydrochloride, a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs.
    Thalidomide-O-amido-PEG4-C2-NH2 hydrochloride
  • HY-138782
    Thalidomide-Piperazine-PEG1-COOH 2731007-11-5 99.24%
    Thalidomide-Piperazine-PEG1-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-Piperazine-PEG1-COOH
  • HY-128832
    Nutlin-C1-amido-PEG4-C2-N3 99.19%
    Nutlin-C1-amido-PEG4-C2-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Nutlin 3 based MDM2 ligand and 4-unit PEG linker used in PROTAC technology. Nutlin-C1-amido-PEG4-C2-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.
    Nutlin-C1-amido-PEG4-C2-N3
  • HY-136166
    Thalidomide-NH-PEG3-propionic acid 2138440-82-9 99.72%
    Thalidomide-NH-PEG3-propionic acid is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.
    Thalidomide-NH-PEG3-propionic acid
  • HY-137531
    Pomalidomide-PEG1-C2-COOH 2139348-60-8 99.76%
    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.
    Pomalidomide-PEG1-C2-COOH
  • HY-134591
    Thalidomide-NH-PEG4-COOH 2412056-48-3 98.55%
    Thalidomide-NH-PEG4-COOH is an E3 ligase ligand-linker conjugate which can be used for synthesizing dCBP-1. dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP.
    Thalidomide-NH-PEG4-COOH
  • HY-131880
    Thalidomide-O-C2-acid 2369068-42-6
    Thalidomide-O-C2-acid is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-O-C2-acid
  • HY-133699
    Pomalidomide-PEG4-COOH 2138440-81-8 ≥98.0%
    Pomalidomide-PEG4-COOH is a E3 ligase ligand-linker conjugate. Pomalidomide-PEG4-COOH contains the Pomalidomide based cereblon ligand and 4-unit PEG linker used in PROTAC technology (extracted from patent WO2017184995A1).
    Pomalidomide-PEG4-COOH
  • HY-130951
    Thalidomide-O-C6-COOH 2169266-69-5 99.29%
    Thalidomide-O-C6-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-O-C6-COOH
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