2. Signaling Pathways
  3. PROTAC
  4. E3 Ligase Ligand-Linker Conjugates

E3 Ligase Ligand-Linker Conjugates

E3 Ligase Ligand-Linker Conjugates

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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 Isoform Specific Products:

E3 Ligase Ligand-Linker Conjugates Isoform Comparison
Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-125843
    Pomalidomide-PEG1-C2-N3 2271036-44-1 99.91%
    Pomalidomide-PEG1-C2-N3 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-N3 can be used to design a selective CDK6 PROTAC degrader CP-10. CP-10 induces the degradation of CDK6 with an DC50 of 2.1 nM. Pomalidomide-PEG1-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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
    Pomalidomide-PEG1-C2-N3
  • HY-141012
    Thalidomide-O-PEG4-NHS ester 2411681-88-2 98.23%
    Thalidomide-O-PEG4-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
    Thalidomide-O-PEG4-NHS ester
  • 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-141015
    Pomalidomide-PEG4-azide 2271036-47-4 99.85%
    Pomalidomide-PEG4-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology. Pomalidomide-PEG4-azide 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.
    Pomalidomide-PEG4-azide
  • HY-132208
    Pomalidomide 4'-PEG2-azide 2271036-45-2 99.30%
    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. Pomalidomide 4'-PEG2-azide 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.
    Pomalidomide 4'-PEG2-azide
  • HY-75706
    N-Descyclopropanecarbaldehyde Olaparib 763111-47-3 99.27%
    N-Descyclopropanecarbaldehyde Olaparib is an analogue of Olaparib containing DOTA moiety. N-Descyclopropanecarbaldehyde Olaparib is a CRBN-based ligand for synthesizing novel dual EGFR and PARP PROTAC, DP-C-4. N-Descyclopropanecarbaldehyde Olaparib can be radiolabeled F-18 or fluorophore for positron emission tomography (PET) or optical imaging in several types of tumor.
    N-Descyclopropanecarbaldehyde Olaparib
  • HY-128846A
    Pomalidomide-C2-NH2 hydrochloride 2305369-00-8 99.46%
    Pomalidomide-C2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology.
    Pomalidomide-C2-NH2 hydrochloride
  • 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-131717
    Thalidomide-NH-CH2-COOH 927670-97-1 98.20%
    Thalidomide-NH-CH2-COOH is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-NH-CH2-COOH can be connected to the ligand for protein by a linker to form PROTACs, such as THAL-SNS-032 (HY-123937).
    Thalidomide-NH-CH2-COOH
  • HY-128767
    VH032-PEG3-acetylene 2098799-80-3 98.14%
    VH032-PEG3-acetylene is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology. VH032-PEG3-acetylene is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    VH032-PEG3-acetylene
  • HY-103604A
    (S,R,S)-AHPC-PEG4-NH2 2010159-57-4 99.51%
    (S,R,S)-AHPC-PEG4-NH2 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
  • HY-103602
    (S,R,S)-AHPC-PEG3-NH2 hydrochloride 2097971-11-2 98.20%
    (S,R,S)-AHPC-PEG3-NH2 hydrochloride 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-NH2 hydrochloride
  • HY-126458
    Thalidomide-O-PEG2-propargyl 2098487-52-4 98.26%
    Thalidomide-O-PEG2-propargyl (E3 ligase Ligand-Linker Conjugates 32) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 2-unit PEG linker used in PROTAC technology. Thalidomide-O-PEG2-propargyl is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Thalidomide-O-PEG2-propargyl
  • HY-137531
    Pomalidomide-PEG1-C2-COOH 2139348-60-8 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.
    Pomalidomide-PEG1-C2-COOH
  • HY-126457
    Thalidomide-propargyl 2098487-39-7 99.97%
    Thalidomide-propargyl is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-propargyl can be connected to the ligand for protein by a linker to form the IMiD containing PROTACs. Thalidomide-propargyl is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Thalidomide-propargyl
  • HY-103607
    (S,R,S)-AHPC-PEG2-C4-Cl 1835705-57-1 98.21%
    (S,R,S)-AHPC-PEG2-C4-Cl (VH032-PEG2-C4-Cl) is a conjugate of ligands for E3 and 13-atom-length linker. The connector of linker is Halogen group. (S,R,S)-AHPC-PEG2-C4-Cl incorporates the (S,R,S)-AHPC based VHL ligand and an alkyl/ether-based linker. (S,R,S)-AHPC-PEG2-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.
    (S,R,S)-AHPC-PEG2-C4-Cl
  • HY-103603
    (S,R,S)-AHPC-PEG2-NH2 hydrochloride 2097973-72-1
    (S,R,S)-AHPC-PEG2-NH2 hydrochloride (VH032-PEG2-NH2 hydrochloride) 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 the synthesis of PROTACs.
    (S,R,S)-AHPC-PEG2-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-135250B
    Thalidomide-4-O-C6-NH2 hydrochloride 2245697-88-3 98.53%
    Thalidomide-4-O-C6-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate used in the PROTAC dTAG-13, a degrader of FKBP12F36V and BET.
    Thalidomide-4-O-C6-NH2 hydrochloride
E3 Ligase Ligand-Linker Conjugates Isoform Comparison

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