2. Signaling Pathways
  3. PROTAC
  4. Ligands for E3 Ligase

Ligands for E3 Ligase

E3 ligase-recruiting Moiety

Ligands for E3 Ligase

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A PROTAC (Proteolysis Targeting Chimeric Molecule) is a protein degrader comprised of a ligand for E3 ligase (E3 ligase binder), a linker and a ligand for target protein (target binder). The association between an E3 ligase and a target protein induced by a PROTAC will lead to the transfer of ubiquitin and degradation of the targeted protein.

E3 ligases catalyze the transfer of ubiquitin to targeted proteins and determine the specificity of the proteins. There are hundreds of E3 ligases in cells, but only a limited number of them are successfully used in reported PROTACs, such as VHL (von Hippel-Lindau disease tumor suppressor protein), CRBN (Cereblon), MDM2 (the mouse double minute 2 homologue) and IAP (inhibitor of apoptosis).

Ligands for E3 Ligase Isoform Specific Products:

Ligands for E3 Ligase Isoform Comparison
Cat. No. 상품명 CAS No. Purity 화학구조
  • HY-158301
    MY-1B 2929308-79-0 99.94%
    MY-1B is a covalent inhibitor of the RNA Methyltransferase NSUN2 (IC50: 1.3 μM). MY-1B stereoselectively ligands active-site cysteine residues (C271) of NSUN2. MY-1B can stereoselectively and covalently bind to PSME1, disrupting the proteasome regulatory complex and downregulating the presentation of specific MHC-I subtypes.
    MY-1B
  • HY-120217
    VH032 1448188-62-2 99.43%
    VH032 is a VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. VH032 is a VHL/HIF-1α interaction inhibitor with a KdPROTACs.
    VH032
  • HY-125845
    (S,R,S)-AHPC 1448297-52-6 99.13%
    (S,R,S)-AHPC (VH032-NH2) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells.
    (S,R,S)-AHPC
  • HY-122542B
    PPACK TFA 157379-44-7 99.80%
    PPACK TFA is an orally active, selective molecular glue degrader targeting IKZF2. Through a molecular glue mechanism, PPACK TFA binds to CRBN, recruits IKZF2 to form a ternary complex, and promotes its ubiquitination and proteasomal degradation. This further converts inhibitory regulatory T cells (Treg) into effector-like T cells, enhances CD8+ T cell responses, and modulates the Teff:Treg balance. PPACK TFA also increases the production of the inflammatory cytokine IL-2 and reduces the suppressive activity of Treg. PPACK TFA can be used in cancer immunotherapy research, and exhibits a synergistic effect when combined with immune checkpoint inhibitors such as anti-PD1.
    PPACK TFA
  • HY-146237
    Golcadomide 2379572-34-4 98.04%
    Golcadomide (CC-99282) is a potent and orally active CRBN E3 ligase modulator (CELMoD). Golcadomide interacts with the CRL4 CRBN E3 ubiquitin ligase substrate receptor CRBN, inducing the recruitment and ubiquitin-mediated proteasomal degradation of the transcription factors Ikaros and Aiolos. Golcadomide shows potential for research in cancer-related fields, including chronic lymphocytic leukemia (CLL) and non-Hodgkin lymphoma (NHL).
    Golcadomide
  • HY-W382038
    E3 ligase Ligand 32 2300099-98-1 99.95%
    E3 ligase Ligand 32 (First product in Example 3) is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 32 can be connected to the ligand for protein by a linker to form PROTACs and can be used for the synthesis of PROTAC SMARCA2/4-degrader-29 (HY-162743).
    E3 ligase Ligand 32
  • HY-W077589
    Lenalidomide-5-aminomethyl hydrochloride 1158264-69-7 98.45%
    Lenalidomide-5-aminomethyl hydrochloride is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-5-aminomethyl hydrochloride can be connected to the ligand for protein by a linker to form PROTAC
    Lenalidomide-5-aminomethyl hydrochloride
  • HY-114740
    β-Naphthoflavone 6051-87-2 99.86%
    β-Naphthoflavone is an exogenous aryl hydrocarbon receptor (AHR) ligand. β-Naphthoflavone can activate AHR to participate in various biological processes, including cell growth, differentiation, apoptosis, and metabolism. β-Naphthoflavone has antioxidant activity and can exert its antioxidant function by regulating the activity of antioxidant enzymes. β-Naphthoflavone is also a non-carcinogenic CYP1A inducer and can be used to study aristolochic acid (AAI) induced renal injury.
    β-Naphthoflavone
  • HY-101763A
    (S,R,S)-AHPC monohydrochloride 1448189-80-7 99.83%
    (S,R,S)-AHPC (VH032-NH2; VHL ligand 1) hydrochloride is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein.
    (S,R,S)-AHPC monohydrochloride
  • HY-112078
    (S,R,S)-AHPC-Me 1948273-02-6 99.96%
    (S,R,S)-AHPC-Me (VHL ligand 2) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM.
    (S,R,S)-AHPC-Me
  • HY-159646
    BMS-986397 2564486-44-6 99.76%
    BMS-986397 is a potent, selective, and orally active cereblon-based molecular glue degrader of casein kinase 1α (CK1α). BMS-986397 induces apoptosis and cell cycle arrest in acute myeloid leukemia (AML) cells. BMS-986397 is a promising agent for the investigation of AML and high-risk myelodysplastic syndromes (HR-MDS).
    BMS-986397
  • HY-41547
    Thalidomide 4-fluoride 835616-60-9 99.92%
    Thalidomide 4-fluoride (Cereblon ligand 4) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide 4-fluoride (Cereblon ligand 4) can be connected to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1 (HY-129966).
    Thalidomide 4-fluoride
  • HY-A0003B
    Lenalidomide hemihydrate 847871-99-2 99.98%
    Lenalidomide hemihydrate (CC-5013 hemihydrate), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hemihydrate is an orally active immunomodulator. Lenalidomide hemihydrate (CC-5013 hemihydrate) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide hemihydrate (CC-5013 hemihydrate) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells.
    Lenalidomide hemihydrate
  • HY-103597
    Thalidomide-O-COOH 1061605-21-7 99.85%
    Thalidomide-O-COOH (Cereblon ligand 3) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-O-COOH (Cereblon ligand 3) can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-O-COOH
  • HY-45512
    E3 ligase Ligand 63 2304754-51-4 99.80%
    E3 ligase Ligand 63 is an E3 ligase ligand that can be used to synthesize CDK2 degrader 2 (HY-163815).
    E3 ligase Ligand 63
  • HY-W593975
    CRBN ligand-547 2446913-88-6 99.82%
    CRBN ligand-547 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. CRBN ligand-547 can be linked to a target protein ligand via a linker to form a PROTAC.
    CRBN ligand-547
  • HY-23095
    Thalidomide-5-OH 64567-60-8 98.23%
    Thalidomide-5-OH is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-OH can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-OH
  • HY-42424
    (S,R,S)-AHPC-Me hydrochloride 1948273-03-7 99.95%
    (S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me hydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM.
    (S,R,S)-AHPC-Me hydrochloride
  • HY-W087383
    Thalidomide 5-fluoride 835616-61-0 99.96%
    Thalidomide 5-fluoride is a thalidomide-based Cereblon ligand used to recruit Cereblon protein. Thalidomide 5-fluoride can be linked to target protein ligands (e.g. IRAK4) through a linker to form PROTAC molecules (e.g. PROTAC IRAK4 degrader-1). PROTAC IRAK4 degrader-1 caused <20%, >20-50%, and >50% IRAK4 protein degradation in OCI-LY-10 cells at concentrations of 0.01, 0.1, and 1 μM, respectively.
    Thalidomide 5-fluoride
  • HY-175742
    BMS-986470 3036554-12-5 99.78%
    BMS-986470, a HbF-activating CRBN E3 ligase modulator (CELMoD), is an orally active dual molecular glue degrader targeting ZBTB7A and WIZ. BMS-986470 has potent γ-globin induction activity. BMS-986470 can be used for sickle cell disease (SCD) research.
    BMS-986470
Cat. No. 상품명 / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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