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:

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-KT001
    E3 Ligase Ligand-Linker Conjugate Kit  
    E3 Ligase Ligand-Linker Conjugate Kit is a series of synthesized compounds that incorporate an E3 ligase ligand and a linker used in PROTAC technology.
    E3 Ligase Ligand-Linker Conjugate Kit
  • HY-111997
    VH285-PEG4-C4-Cl 1799506-07-2 ≥98.0%
    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.
    VH285-PEG4-C4-Cl
  • HY-103599
    (S,R,S)-AHPC-PEG2-N3 2010159-45-0 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.
    (S,R,S)-AHPC-PEG2-N3
  • HY-112495
    VH032-PEG5-C6-Cl 1799506-06-1 99.76%
    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.
    VH032-PEG5-C6-Cl
  • 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-103601
    (S,R,S)-AHPC-PEG4-N3 1797406-81-5 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.
    (S,R,S)-AHPC-PEG4-N3
  • HY-W580022
    Pomalidomide-5'-PEG8-C2-COOH 2138440-78-3 98.21%
    Pomalidomide-5'-PEG8-C2-COOH is an E3 Ligase Ligand-Linker Conjugates, consisting of Pomalidomide (HY-10984) and a linker. Pomalidomide-5'-PEG8-C2-COOH can be used for synthesis of PROTACs.
    Pomalidomide-5'-PEG8-C2-COOH
  • HY-131878
    Pomalidomide-C7-NH2 hydrochloride 2446474-05-9 98.98%
    Pomalidomide-C7-NH2 (Pomalidomide 4'-alkylC7-amine) hydrochloride is an E3 ligase ligand-linker conjugate. Pomalidomide-C7-NH2 hydrochloride can be used for the synthesis of PROTAC.
    Pomalidomide-C7-NH2 hydrochloride
  • HY-W584518
    Thalidomide-5-O-CH2-COOH 2467425-53-0
    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.
    Thalidomide-5-O-CH2-COOH
  • HY-130271
    (S,R,S)-AHPC-PEG5-COOH 2172820-14-1 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.
    (S,R,S)-AHPC-PEG5-COOH
  • HY-103598
    (S,R,S)-AHPC-PEG3-N3 1797406-80-4 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.
    (S,R,S)-AHPC-PEG3-N3
  • HY-131872
    Pomalidomide-PEG2-COOH 2140807-17-4 99.87%
    Pomalidomide-PEG2-COOH (Pomalidomide 4'-PEG2-acid) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 2-unit PEG linker used in PROTAC technology.
    Pomalidomide-PEG2-COOH
  • 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-103600
    (S,R,S)-AHPC-PEG1-N3 2101200-09-1 98.18%
    (S,R,S)-AHPC-PEG1-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 1-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-PEG1-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.
    (S,R,S)-AHPC-PEG1-N3
  • 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-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-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-141015
    Pomalidomide-PEG4-azide 2271036-47-4
    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-141431
    Cbl-b-IN-2 2503325-21-9
    Cbl-b-IN-2 (Example 8) is an orally bioavailable compound, can inhibit the E3 enzyme Casitas B-lineage lymphoma proto-oncogene-b (Cbl-b) in the ubiquitin proteasome pathway. Cbl-b-IN-2 can be used to modulate the immune system and diseases amenable to immune system modulation. Cbl-b-IN-2 (Example 8) also may be administered to an individual with cancer, either alone or as part of a combination, with one or more of an immune checkpoint inhibitor, an anti-neoplastic agent, and radiation agent.
    Cbl-b-IN-2
  • 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-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
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