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  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. Nombre del producto No. CAS Pureza Estructura química
  • HY-W093272
    Thalidomide-5,6-F 1496997-41-1 99.84%
    Thalidomide-5,6-F is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5,6-F can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5,6-F
  • HY-W013021
    Norbornene 498-66-8 99.95%
    Norbornene is a cycloolefin and building block for synthesis of porous organic polymeric materials via metathesis, addition, and CANAL polymerization. Norbornene can also be used as an E3 ligase ligand for the synthesis of PROTAC, such as PROTAC HyTTD Degrader-1 (HY-181895).
    Norbornene
  • HY-149935
    OICR-8268 3000549-26-5 99.23%
    OICR-8268 is a reversible DCAF1 ligand that binds to the DCAF1 WDR domain with a Kd of 38 nM. OICR-8268 can enable the development of DCAF1-based PROTACs.
    OICR-8268
  • HY-W1004786
    CRBN ligand-13 3050687-70-9
    CRBN ligand-13 is a CRBN-type E3 ubiquitin ligase ligand that can be used to prepare PROTAC.
    CRBN ligand-13
  • HY-150839
    E3 ligase Ligand PG 14149-34-9 99.94%
    E3 ligase Ligand PG is a E3 ligase ligand that can be used in the recruitment of CRBN protein. E3 ligase Ligand PG exhibits potent binding activity with CRBN (IC50 of 2.191 μM). E3 ligase Ligand PG can be connected to the BMS-202 (HY-19745) by a linker to form PROTAC, PROTAC PD-L1 degrader-1 (HY-163757).
    E3 ligase Ligand PG
  • HY-W023573
    5-Aminothalidomide 191732-76-0 99.69%
    5-Aminothalidomide is an E3 ligase ligand used in PROTAC technology. 5-Aminothalidomide can be used to synthesize various PROTACs, such as the PROTAC BRD9 Degrader-7 (HY-155361).
    5-Aminothalidomide
  • HY-W243404
    3-(6-Bromo-1-oxoisoindolin-2-yl)piperidine-2,6-dione 2304513-76-4 99.95%
    3-(6-Bromo-1-oxoisoindolin-2-yl)piperidine-2,6-dione is a Lenalidomide analog that can be useful in PROTAC research.
    3-(6-Bromo-1-oxoisoindolin-2-yl)piperidine-2,6-dione
  • HY-42419
    (S,R,S)-AHPC-Me-NHBoc 1997302-16-5 98.26%
    (S,R,S)-AHPC-Me-NHBoc is an E3 ubiquitin ligase VHL ligand used to recruit the VHL protein. (S,R,S)-AHPC-Me-NHBoc can be linked to a target protein ligand via a linker to form a PROTAC.
    (S,R,S)-AHPC-Me-NHBoc
  • HY-W243100
    5-Br-6-F-Desamino lenalidomide 2409005-96-3
    5-Br-6-F-Desamino lenalidomide is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. 5-Br-6-F-Desamino lenalidomide can be linked to a target protein ligand via a linker to form a PROTAC.
    5-Br-6-F-Desamino lenalidomide
  • HY-W093472
    Desamino lenalidomide-6-COOH 2171780-01-9 98.45%
    Desamino lenalidomide-6-COOH is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. Desamino lenalidomide-6-COOH can be linked to a target protein ligand via a linker to form a PROTAC.
    Desamino lenalidomide-6-COOH
  • HY-133144
    Lenalidomide-OH 1416990-08-3 99.48%
    Lenalidomide-OH is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein. Lenalidomide-OH can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC BTK degrader SJF620 (HY-133137).
    Lenalidomide-OH
  • HY-139539
    Thalidomide-5-COOH 1216805-11-6 99.94%
    Thalidomide-5-COOH is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-COOH can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-COOH
  • HY-W037495
    DCAF15 ligand-1 2098346-67-7 99.32%
    DCAF15 ligand-1 (compound 9) is a ligand for the E3 ligase DCAF15. DCAF15 ligand-1 can be used in the synthesis of IBG1 (HY-153459).
    DCAF15 ligand-1
  • HY-W761299
    PD 4'-oxyacetic acid 2633633-12-0 99.69%
    PD 4'-oxyacetic acid is a carboxylic acid-functionalized cereblon ligand that can be used for PROTAC Degrader development.
    PD 4'-oxyacetic acid
  • HY-W576870
    Hydrouracil-3-Ph-COOH 2377644-59-0 98.91%
    Hydrouracil-3-Ph-COOH is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. Hydrouracil-3-Ph-COOH can be linked to a target protein ligand via a linker to form a PROTAC.
    Hydrouracil-3-Ph-COOH
  • HY-W460193
    N-Me-Thalidomide 4-fluoride 2244520-92-9 99.41%
    N-Me-Thalidomide 4-fluoride is a ligand for E3 ligase, used for the synthesis of Anti-inflammatory agent 70 (HY-157570).
    N-Me-Thalidomide 4-fluoride
  • HY-157566
    Lenalidomide 5'-piperazine-4-methylpiperidine hydrochloride 2520105-60-4 98.57%
    Lenalidomide 5'-piperazine-4-methylpiperidine hydrochloride is a functionalized cerebellar ligand for PROTAC development, combining E3 ligand and terminal piperidine for subsequent chemical reactions. A protein degradant with a rigid connector is generated.
    Lenalidomide 5'-piperazine-4-methylpiperidine hydrochloride
  • HY-W259932
    Lenalidomide 5'-piperazine hydrochloride 2222120-31-0 99.92%
    Lenalidomide 5'-piperazine hydrochloride can serve as a Cereblon ligand to recruit CRBN protein. Lenalidomide 5'-piperazine hydrochloride can be linked to target protein ligands via a linker to form PROTAC molecules, such as KI-CDK9d-32 (HY-173523).
    Lenalidomide 5'-piperazine hydrochloride
  • HY-42424A
    (S,R,S)-AHPC-Me dihydrochloride 2504950-56-3 99.84%
    (S,R,S)-AHPC-Me dihydrochloride (VHL ligand 2 dihydrochloride) 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 dihydrochloride 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 dihydrochloride
  • HY-111663
    VL285 1448188-57-5 99.34%
    VL285 is a potent VHL ligand with an IC50 of 0.34 μM.
    VL285
Cat. No. Nombre del producto / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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