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-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-145449
    CC-885-CH2-PEG1-NH-CH3 2722698-03-3 99.22%
    CC-885-CH2-PEG1-NH-CH3 is a neoDegrader that can be used in the synthesis of Antibody neoDegrader Conjugate (AnDC).
    CC-885-CH2-PEG1-NH-CH3
  • HY-145448
    MC-VC-PABC-amide-PEG1-CH2-CC-885 2722697-82-5 99.57%
    MC-VC-PABC-amide-PEG1-CH2-CC-885 (compound III) is a neoDegrader, a conjugate of the GSPT1 degrader/molecular glue CC-885 (HY-101488) and a linker. MC-VC-PABC-amide-PEG1-CH2-CC-885 can be conjugated to the antibody DAR3.7 that specifically targets CD56 to synthesize Antibody-Drug Conjugates (ADCs). MC-VC-PABC-amide-PEG1-CH2-CC-885 can also be conjugated to Belantamab (HY-P9980), Daratumumab (HY-P9915), huMy9-6 IgG1, Indatuximab (HY-P990607), Isatuximab (HY-P9976), lintuzumab IgG1, Pertuzumab (HY-P9912), OR000213, Rituximab (HY-P9913), Sacituzumab (HY-P99045), Trastuzumab (HY-P9907)and U3-1784 (HY-P990672) to form conjugates.
    MC-VC-PABC-amide-PEG1-CH2-CC-885
  • HY-130271
    (S,R,S)-AHPC-PEG5-COOH 2172820-14-1 99.80%
    (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. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
    (S,R,S)-AHPC-PEG3-N3
  • HY-159548
    Cyclopropane-(S,R,S)-AHPC-CO-cyclohexene-Bpin
    SMARCA2/4-ligand-Linker Conjugate-3 is an E3 ligase ligand-linker conjugate.
    Cyclopropane-(S,R,S)-AHPC-CO-cyclohexene-Bpin
  • HY-161793
    (S,R,S)-AHPC-NHCO-C-O-C5-N3 2816967-28-7
    (S,R,S)-AHPC-NHCO-C-O-C5-N3 is a conjugate of ligand for E3 ligase (HY-125845) and linker (HY-161792). (S,R,S)-AHPC-NHCO-C-O-C5-N3 can be utilized for synthesis of PROTAC SARS-CoV-2 Mpro degrader-3 (HY-161789).
    (S,R,S)-AHPC-NHCO-C-O-C5-N3
  • HY-162546
    3-Hydroxypropanoic acid-pip-hydroquinone-dihydrouracil
    3-hydroxypropanoic acid-pip-hydroquinone-dihydrouracil is a conjugate of E3 ligase ligand and linker that serve as a key intermediate for the synthesis of complete PROTAC HPK1 Degrader-2 (HY-162544).
    3-Hydroxypropanoic acid-pip-hydroquinone-dihydrouracil
  • HY-103601
    (S,R,S)-AHPC-PEG4-N3 1797406-81-5 99.93%
    (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. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
    (S,R,S)-AHPC-PEG4-N3
  • 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-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. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
    Pomalidomide-PEG1-C2-N3
  • HY-112495
    VH032-PEG5-C6-Cl 1799506-06-1 99.93%
    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-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. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
    (S,R,S)-AHPC-PEG1-N3
  • HY-141012
    Thalidomide-O-PEG4-NHS ester 2411681-88-2
    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-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-103602
    (S,R,S)-AHPC-PEG3-NH2 hydrochloride 2097971-11-2 99.01%
    (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-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-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. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
    (S,R,S)-AHPC-PEG2-N3
  • HY-152231
    BODIPY FL thalidomide 2740620-18-0 99.20%
    BODIPY FL thalidomide is a high-affinity fluorescent probe for the human cereblon protein with a Kd value of 3.6 nM[1]
    BODIPY FL thalidomide
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
E3 Ligase Ligand-Linker Conjugates Isoform Comparison

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