PROTAC

PROTAC(蛋白降解靶向嵌合体)

The PROTAC molecule itself contains three distinct portions: a ligand for binding to the target protein, a ligand for binding to an E3 ligase, and a linker joining these two ligands.

PROTACs (proteolysis-targeting chimaeras) are bifunctional molecules that bring a target protein into spatial proximity with an E3 ubiquitin ligase to trigger target ubiquitination and subsequent proteasomal degradation. Effective redirection of ligase poly-ubiquitination activity toward a new substrate protein requires formation of a ligase:PROTAC:target ternary complex, an intermediate species that is crucial to the cellular activity of degrader molecules. A characteristic feature of PROTACs mode of action is their sub-stoichiometric catalytic activity that alleviates the requirement for target engagement and occupancy of traditional inhibitors. New PROTAC molecules designed guided by the crystal structure show exquisite selectivity for inducing cellular depletion of Brd4 over its BET family members Brd2 and Brd3.

PROTAC 相关产品(146)

  • GC50630 structure
    GC50630aTAG 2139
    CAS: 2387510-81-6

    Degrader of MTH1 fusion proteins for use within the aTAG system

  • GC50631 structure
    GC50631aTAG 4531
    CAS: 2412985-00-1

    Degrader of MTH1 fusion proteins for use within the aTAG system

  • GC50634 structure
    GC50634VH 032 amide-alkylC5-amine
    CAS: 2415256-20-9

    VHL ligand with alkyl linker and terminal amine for onward chemistry

  • GC50646 structure
    GC50646VH 032 amide-alkylC7-amine

    VHL ligand with alkyl linker and terminal amine for onward chemistry

  • GC50652 structure
    GC50652xStAx-VHLL
    纯度: >95.00%

    Selective peptide-based β-catenin Degrader

  • GC50658 structure
    GC50658Pomalidomide 4'-alkylC3-amine
    CAS: 2154342-45-5
    纯度: >95.00%

    Pomalidomide 4'-alkylC3-amine 是一种合成的 E3 连接酶配体-接头偶联物,它包含基于 Pomalidomide 的 cereblon 配体和 PROTAC 技术中使用的接头。

  • GC50665 structure
    GC50665Pomalidomide 4'-alkylC3-acid
    CAS: 2225940-47-4
    纯度: >95.00%

    Functionalized cereblon ligand for research and development; incorporates an E3 ligase ligand plus an alkylC3 linker with terminal acid ready for conjugation to a target protein ligand

  • GC50669 structure
    GC50669Lenalidomide 4'-PEG1-amine
    CAS: 2624336-86-1
    纯度: >95.00%

    Functionalized cereblon ligand for PROTAC® research and development; incorporates an E3 ligase ligand plus a PEG1 linker with terminal amine ready for conjugation to a target protein ligand

  • GC50674 structure
    GC50674Pomalidomide 4'-alkylC4-acid
    CAS: 2225940-48-5
    纯度: >95.00%

    Functionalized cereblon ligand for PROTAC(R) research and development; incorporates an E3 ligase ligand plus an alkylC4 linker with terminal acid ready for conjugation to a target protein ligand

  • GC50675 structure
    GC50675Pomalidomide 4'-PEG1-acid
    CAS: 2139348-60-8
    纯度: >99.50%

    Pomalidomide 4'-PEG1-acid 是一种合成的 E3 连接酶配体-接头偶联物,它结合了 PROTAC 技术中使用的基于 Pomalidomide 的 cereblon 配体和 1 单位 PEG 接头。

  • GC50684 structure
    GC50684Lenalidomide 4'-PEG2-amine
    CAS: 2624336-88-3
    纯度: >95.00%

    Functionalized cereblon ligand for PROTAC® research and development; incorporates an E3 ligase ligand plus a PEG2 linker with terminal amine ready for conjugation to a target protein ligand

  • GC50689 structure
    GC50689Pomalidomide 4'-alkylC6-acid
    CAS: 2225940-50-9
    纯度: >95.00%

    Functionalized cereblon ligand for PROTAC(R) research and development; incorporates an E3 ligase ligand plus an alkylC6 linker with terminal acid ready for conjugation to a target protein ligand

  • GC50690 structure
    GC50690Pomalidomide 4'-PEG2-acid
    CAS: 2140807-17-4
    纯度: >95.00%

    Pomalidomide 4'-PEG2-acid (Pomalidomide 4'-PEG2-acid) 是一种合成的 E3 连接酶配体-接头偶联物,它包含基于 Pomalidomide 的 cereblon 配体和用于 PROTAC 技术的 2 单元 PEG 接头。

  • GC50694 structure
    GC50694Lenalidomide 4'-PEG3-amine
    CAS: 2624336-87-2
    纯度: >95.00%

    Functionalized cereblon ligand for PROTAC® research and development; incorporates an E3 ligase ligand plus a PEG3 linker with terminal amine ready for conjugation to a target protein ligand

  • GC50696 structure
    GC50696Pomalidomide 4'-alkylC8-acid
    CAS: 2305936-70-1
    纯度: >95.00%

    Functionalized cereblon ligand for PROTAC(R) research and development; incorporates an E3 ligase ligand plus an alkylC8 linker with terminal acid ready for conjugation to a target protein ligand

  • GC50698 structure
    GC50698VH 032, amine
    CAS: 2137142-47-1
    纯度: >98.00%

    Derivative of the von Hippel-Lindau (VHL) ligand, VH 032; commonly used as a precursor to a PROTAC® that hijacks VHL as the E3 ubiquitin ligase component

  • GC50705 structure
    GC50705Pomalidomide 4'-PEG4-acid
    CAS: 2138440-81-8
    纯度: >95.00%

    Pomalidomide-PEG4-COOH 是一种 E3 连接酶配体-接头偶联物,包含基于 Pomalidomide 的 cereblon 配体和用于 PROTAC 技术的 4 单元 PEG 接头。

  • GC50709 structure
    GC50709Thalidomide 4'-oxyacetamide-alkylC1-PEG3-alkylC3-amine
    CAS: 2564466-93-7
    纯度: >95.00%

    Functionalized cereblon ligand for PROTAC® research and development; incorporates an E3 ligase ligand plus an alkylC1-PEG3-alkylC3 linker with terminal amine ready for conjugation to a target protein ligand

  • GC50712 structure
    GC50712VH 032 amide-alkylC2-acid
    CAS: 2172819-72-4
    纯度: >95.00%

    Functionalized von-Hippel-Lindau protein ligand (VHL) for PROTAC® research and development; incorporates an E3 ligase ligand plus alkylC2 linker with terminal carboxylic acid ready for conjugation to a target protein ligand

  • GC50714 structure
    GC50714VH 032 amide-alkylC3-amine
    CAS: 2564467-25-8
    纯度: >95.00%

    Functionalized von-Hippel-Lindau (VHL) protein ligand for PROTAC® research and development; incorporates an E3 ligase ligand plus an alkyl C3 linker and terminal amine ready for conjugation to a target protein ligand

  • GC50718 structure
    GC50718VH 032 amide-alkylC3-acid
    CAS: 2172819-73-5
    纯度: >95.00%

    Functionalized von-Hippel-Lindau protein ligand (VHL) for research and development; incorporates an E3 ligase ligand plus alkylC3 linker with terminal carboxylic acid ready for conjugation to a target protein ligand

  • GC50720 structure
    GC50720VH 032 amide-PEG1-acid
    CAS: 2172820-07-2
    纯度: >95.00%

    Functionalized von-Hippel-Lindau (VHL) protein ligand for PROTAC® research and development; incorporates an E3 ligase ligand plus a PEG1 linker with terminal carboxylic acid ready for conjugation to a target protein ligand

  • GC50723 structure
    GC50723VH 101 phenol-alkylC4-amine
    CAS: 2564467-03-2
    纯度: >95.00%

    Functionalized von-Hippel-Lindau protein ligand (VHL) for PROTAC® research and development; incorporates an E3 ligase ligand plus an alkylC4 linker with terminal amine ready for conjugation to a target protein ligand

  • GC50724 structure
    GC50724VH 032 amide-alkylC6-acid
    CAS: 2172819-75-7
    纯度: >95.00%

    Functionalized von-Hippel-Lindau protein ligand (VHL) for PROTAC® research and development; incorporates an E3 ligase ligand plus alkylC6 linker with terminal carboxylic acid ready for conjugation to a target protein ligand