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-103608
    (S,R,S)-AHPC-(C3-​PEG)​2-​C6-​Cl 1835705-61-7 99.89%
    (S,R,S)-AHPC-(C3-​PEG)​2-​C6-​Cl is a small molecule HaloPROTAC that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker. (S,R,S)-AHPC-(C3-​PEG)​2-​C6-​Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.
    (S,R,S)-AHPC-(C3-​PEG)​2-​C6-​Cl
  • HY-131866
    (S,R,S)-CO-C2-acid 2172819-72-4 98.0%
    (S,R,S)-CO-C2-acid (VH 032 amide-alkylC2-acid) is a functionalized von-Hippel-Lindau (VHL) protein ligand that can be used in PROTAC research and development. (S,R,S)-CO-C2-acid contains an E3 ligand alkyl ligand for conjugation of target protein ligands.
    (S,R,S)-CO-C2-acid
  • HY-167759
    Pomalidomide-PEG2-acetic acid 2143097-05-4 99.43%
    Pomalidomide-PEG2-acetic acid (Pomalidomide-PEG2-CH2COOH) is the conjugate composed of a E3 ligase ligand and a linker. Pomalidomide-PEG2-acetic acid can be used for PROTAC synthesis.
    Pomalidomide-PEG2-acetic acid
  • HY-145615
    Pomalidomide-C12-NH2 hydrochloride 2862774-02-3
    Pomalidomide-C12-NH2 hydrochloride is the E3 ligase ligand-linker conjugate of PROTAC KRAS G12C degrader-1 (HY-139186). PROTAC KRAS G12C degrader-1 is a Cereblon-based KRASG12C degrader.
    Pomalidomide-C12-NH2 hydrochloride
  • HY-136187A
    (S,R,S)-AHPC-C5-NH2 dihydrochloride 2415256-20-9
    (S,R,S)-AHPC-C5-NH2 (VH032-C5-NH2) dihydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for estrogen-related receptor α (ERRα) PROTAC degrader.
    (S,R,S)-AHPC-C5-NH2 dihydrochloride
  • HY-169357
    Acepromazine-1-Piperazinepropanamine
    Acepromazine-1-Piperazinepropanamine (compound 10) is a synthesized E3 ligase ligand-linker conjugate (E3 Ligase Ligand-Linker Conjugate) that incorporates a TRIM21 ligand and a linker. Acepromazine-1-Piperazinepropanamine can be connected to the target protein ligand to form a PROTAC molecule, TrimTAC1 (HY-169355).
    Acepromazine-1-Piperazinepropanamine
  • HY-163167
    VH 032 amide-alkylC5-azide 2821804-11-7 98.32%
    VH 032 amide-alkylC5-amine is a functionalized von-Hippel-Lindau protein ligand (VHL) for PROTAC research and development; incorporates an E3 ligase ligand plus an alkyl linker with terminal amine ready for conjugation to a target protein ligand.
    VH 032 amide-alkylC5-azide
  • HY-115560A
    Thalidomide-O-amido-C3-NH2 TFA 2022182-58-5 99.58%
    Thalidomide-O-amido-C3-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-O-amido-C3-NH2 TFA
  • HY-130617
    Pomalidomide-amido-C1-Br 2351106-38-0
    Pomalidomide-amido-C1-Br is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker. Pomalidomide-amido-C1-Br can be used to design a B-Raf PROTAC degrader PROTAC B-Raf degrader 1 (HY-111758). PROTAC B-Raf degrader 1 has anti-cancer activity.
    Pomalidomide-amido-C1-Br
  • HY-131959
    (S,R,S)-AHPC-PEG5-Boc 2923734-82-9
    (S,R,S)-AHPC-PEG5-Boc is a E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used for Cdc20 degrader CP5V.
    (S,R,S)-AHPC-PEG5-Boc
  • HY-136165
    (S,R,S)-AHPC-PEG3-propionic acid 2140807-42-5
    (S,R,S)-AHPC-PEG3-propionic acid 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-propionic acid
  • HY-130854
    Thalidomide-NH-C6-NH-Boc 2093536-13-9
    Thalidomide-NH-C6-NH-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used for MI-389 (compound 22) synthesis. MI-389 is a potent phthalimide PROTAC degrader based on the multi-targeted receptor tyrosine kinase inhibitor sunitinib (HY-10255A).
    Thalidomide-NH-C6-NH-Boc
  • HY-112617A
    Thalidomide-O-amido-PEG2-C2-NH2 TFA 1957235-75-4 99.72%
    Thalidomide-O-amido-PEG2-C2-NH2 TFA 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-amido-PEG2-C2-NH2 TFA
  • HY-107438
    Thalidomide-O-amido-C4-NH2 1799711-24-2
    Thalidomide-O-amido-C4-NH2 (Cereblon Ligand-Linker Conjugates 6), 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-C4-NH2
  • HY-130682
    Lenalidomide-propargyl-C2-amido-Ph-NH2 hydrochloride 2748150-20-9
    Lenalidomide-propargyl-C2-amido-Ph-NH2 hydrochloride incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase and a linker. Lenalidomide-propargyl-C2-amido-Ph-NH2 hydrochloride can be used to design the PROTAC MD-224 (HY-114312). Lenalidomide-propargyl-C2-amido-Ph-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-amido-Ph-NH2 hydrochloride
  • HY-136160
    Thalidomide 4'-oxyacetamide-alkyl-C2-amine hydrochloride 2341841-02-7 99.12%
    Thalidomide 4'-oxyacetamide-alkyl-C2-amine hydrochloride incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase, and a linker. Thalidomide 4'-oxyacetamide-alkyl-C2-amine hydrochloride can be used to design the PROTACs.
    Thalidomide 4'-oxyacetamide-alkyl-C2-amine hydrochloride
  • HY-136006A
    (S,R,S)-AHPC-C6-NH2 hydrochloride 2360522-76-3
    (S,R,S)-AHPC-C6-NH2 hydrochloride (VH032-C6-NH2 hydrochloride) 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-C6-NH2 hydrochloride is XF038-161A, example 6, extracted from patent WO2019173516A1.
    (S,R,S)-AHPC-C6-NH2 hydrochloride
  • HY-136055
    (S,R,S)-AHPC-C5-COOH 2267282-19-7 98.81%
    (S,R,S)-AHPC-C5-COOH (VH032-C5-COOH) is a synthesized E3 ligase ligand-linker conjugate, contains the VH032 VHL-based ligand and a linker to form PROTACs. VH-032 is a selective and potent inhibitor of VHL/HIF-1α interaction with a Kd of 185 nM, has the potential for the study of anemia and ischemic diseases.
    (S,R,S)-AHPC-C5-COOH
  • HY-138789
    Thalidomide-Piperazine-PEG1-NH2 2357111-29-4
    Thalidomide-Piperazine-PEG1-NH2 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-NH2
  • HY-129704A
    Thalidomide-NH-C6-NH2 TFA 2093386-51-5 99.82%
    Thalidomide-NH-C6-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-NH-C6-NH2 TFA
Cat. No. Product Name / Synonyms Application Reactivity
E3 Ligase Ligand-Linker Conjugates Isoform Comparison

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