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-136269
    A 410099.1, amine-Boc hydrochloride 2374122-37-7 99.71%
    A 410099.1, amine-Boc hydrochloride is a functionalized IAP ligand and can be used for the synthesis of PROTACs, such as PROTACs targeting BTK (PROTACs 4 and 5).
    A 410099.1, amine-Boc hydrochloride
  • HY-129703B
    Thalidomide-PEG2-C2-NH2 hydrochloride 2245697-87-2 99.93%
    Thalidomide-PEG2-C2-NH2 hydrochloride 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-PEG2-C2-NH2 hydrochloride
  • 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. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
    Pomalidomide-PEG4-azide
  • HY-161128
    Lenalidomide 4'-PEG1-amine dihydrochloride 2624336-86-1 99.51%
    Lenalidomide 4'-PEG1-amine dihydrochloride is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide 4'-PEG1-amine dihydrochloride can be connected to the ligand for protein by a linker to form PROTAC.
    Lenalidomide 4'-PEG1-amine dihydrochloride
  • HY-131872
    Pomalidomide-PEG2-COOH 2140807-17-4 99.86%
    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-139345
    (S,R,S)-AHPC-CO-C9-acid 2172819-78-0
    (S,R,S)-AHPC-CO-C9-acid is an E3 ligase ligand-linker conjugate that can be connected to the ligand for protein to form PROTACs.
    (S,R,S)-AHPC-CO-C9-acid
  • HY-130271
    (S,R,S)-AHPC-PEG5-COOH 2172820-14-1 99.79%
    (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-141011
    Thalidomide-O-amido-PEG4-azide 2411681-89-3 99.19%
    Thalidomide-O-amido-PEG4-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Thalidomide-O-amido-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. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
    Thalidomide-O-amido-PEG4-azide
  • HY-122725B
    Lenalidomide-C5-NH2 hydrochloride 2595367-27-2 99.28%
    Lenalidomide-C5-NH2 hydrochloride is an E3 ligase ligand-linker conjugate. Lenalidomide-C5-NH2 hydrochloride can be coupled to a target protein ligand via a linker to form a PROTAC molecule—such as a PROTAC degrader for MDM2.
    Lenalidomide-C5-NH2 hydrochloride
  • HY-128767
    VH032-PEG3-acetylene 2098799-80-3 98.10%
    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-130652
    Pomalidomide 4'-PEG3-azide 2271036-46-3
    Pomalidomide 4'-PEG3-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide-based cereblon ligand and a linker. Pomalidomide 4'-PEG3-azide can be used for the synthesis of iRucaparib-TP3 (Compound 3). iRucaparib-TP3 is a highly efficient PARP1?degrader based on Rucaparib by using the PROTAC approach. Pomalidomide 4'-PEG3-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. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
    Pomalidomide 4'-PEG3-azide
  • 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-115446A
    Lenalidomide-C4-NH2 hydrochloride 2435715-90-3
    Lenalidomide-C4-NH2 hydrochloride is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C4-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTAC (Compound 24), which has IC50s of 0.98 nM and 13.7 nM in inhibition of RS4;11 and MOLM-13 acute leukemia cell lines growth, respectively.
    Lenalidomide-C4-NH2 hydrochloride
  • HY-148671
    (S,R,S)-AHPC-amido-C7-acid 2172819-76-8 98.71%
    (S,R,S)-AHPC-amido-C7-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 PROTACs.
    (S,R,S)-AHPC-amido-C7-acid
  • HY-W854844A
    (E)-JP-2-196 TFA 3065021-33-9
    JP-2-196 (TFA) is a molecular glue handle that can bind to the E3-ubiquitin ligases (RNF126, LRSAM1, RNF40, MID2, and RNF14) in vitro. JP-2-196 (TFA) can be used to synthesize molecular glue degraders.
    (E)-JP-2-196 TFA
  • HY-101460
    Tz-Thalidomide 2087490-42-2 98.60%
    Tz-Thalidomide is a tetrazine-tagged Thalidomide (HY-14658), an E3 ligase ligand. Tz-Thalidomide self-assembles with TCO-labeled target protein inhibitors, forming a CLIP-TAC (targeted protein degradation chimera) via click chemistry. This chimera recruits the E3 ubiquitin ligase CRBN to the target protein, thereby inducing ubiquitination and subsequent degradation of the target protein. When used in combination with JQ1-TCO (HY-148864), Tz-Thalidomide induces concentration-dependent degradation of BRD4 in cells. When combined with ERK-targeting protein inhibitors, Tz-Thalidomide induces degradation of ERK1/2 in cells. Tz-Thalidomide can be used in cancer-related research.
    Tz-Thalidomide
  • 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
  • HY-46531
    Thalidomide-5-NH2-CH2-COOH 2412056-27-8
    Thalidomide-5-NH2-CH2-COOH (compound 114) is a potent and selective inhibitor of tropomyosin receptor kinase (trk). Thalidomide-5-NH2-CH2-COOH is a ligand of E3 ligase. Thalidomide-5-NH2-CH2-COOH has the potential for researching one or more diseases (extracted from patent WO2021170109A1).
    Thalidomide-5-NH2-CH2-COOH
  • 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-148142
    Pomalidomide-C3-NHS ester 2828476-87-3 98.70%
    Pomalidomide-C3-NHS ester is a synthesized E3 ligase ligand-linker conjugate, incorporating the Pomalidomide based cereblon ligand and NHS ester linker.
    Pomalidomide-C3-NHS ester
Cat. No. Product Name / Synonyms Application Reactivity
E3 Ligase Ligand-Linker Conjugates Isoform Comparison

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