GlpBio

PROTAC

PROTAC(蛋白降解靶向嵌合体)

PROTACs or Proteolysis Targeting Chimeric Molecules are heterobifunctional nanomolecules that theoretically target any protein for ubiquitination and degradation. In terms of the structure, PROTACs consist of one moiety which is recognized by the E3 ligase. This moiety is then chemically and covalently linked to a small molecule or a protein that recognizes the target protein. The trimeric complex formation leads to the transfer of ubiquitins to the target protein.

By removing target proteins directly rather than merely blocking them, PROTACs can provide multiple advantages over small molecule inhibitors, which can require high systemic exposure to achieve sufficient inhibition, often resulting in toxic side effects and eventual drug resistance. PROTAC molecules possess good tissue distribution and the ability to target intracellular proteins, thus can be directly applied to cells or injected into animals without the use of vectors.

Targeted protein degradation using the PROTAC technology is emerging as a novel therapeutic method to address diseases, such as cancer, driven by the aberrant expression of a disease-causing protein. In addition to the use of PROTACs for the treatment of human disease, these molecules provide a chemical genetic approach to “knock down” proteins to study their function. Currently, there are several small molecule inhibitors that have been found to show good biological activity by specifically targeting BET, estrogen receptor (ER), androgen receptor, etc.

References:

[1] Sakamoto KM. Pediatr Res. 2010 May;67(5):505-8.

[2] Neklesa TK, et al. Pharmacol Ther. 2017 Jun;174:138-144.

研究方向

PROTAC 相关产品(250)

  • 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

  • GC50729 structure
    GC50729VH 101 phenol-alkylC6-amine
    CAS: 2564467-16-7
    纯度: >95.00%

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

  • GC50730 structure
    GC50730VH 032 amide-alkylC8-acid
    CAS: 2172819-77-9
    纯度: >95.00%

    Functionalized von-Hippel-Lindau protein ligand (VHL) for PROTAC® research and development; incorporates an E3 ligase ligand plus alkylC8 linker with terminal carboxylic acid ready for conjugation to a target protein ligand

  • GC50731 structure
    GC50731VH 032 amide-PEG4-amine
    CAS: 2446474-04-8
    纯度: >95.00%

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

  • GC50736 structure
    GC50736dBRD9-A
    CAS: 2170679-42-0
    纯度: >98.00%

    Potent BRD9 degrader

  • GC50737 structure
    GC50737A 410099.1 amide-PEG4-amine
    CAS: 2446474-10-6
    纯度: >95.00%

    Functionalized IAP ligand for PROTAC® research and development; incorporates an IAP ligand plus an amide-PEG4 linker with terminal amine ready for conjugation to a target protein ligand