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)

  • GC39264 structure
    GC39264FKBP12 PROTAC dTAG-13
    CAS: 2064175-41-1
    纯度: >99.50%

    FKBP12 PROTAC dTAG-13 (dTAG-13) 是一种基于 PROTAC 的双功能降解剂。FKBP12 PROTAC dTAG-13 (dTAG-13) 既是一种 FKBP12F36V 的降解剂，又是一种选择性的 BET BRD4 降解剂，FKBP12 PROTAC dTAG-13 (dTAG-13) 通过将 BET 溴结构域桥接至 E3 泛素连接酶 (cereblon; CRBN) 而形成降解剂。

  • GC39289 structure
    GC39289FKBP12 PROTAC dTAG-7
    CAS: 2064175-32-0
    纯度: >98.00%

    FKBP12 PROTAC dTAG-7 (dTAG-7) 是一种双功能降解剂。FKBP12 PROTAC dTAG-7 (dTAG-7) 既是一种 FKBP12F36V 的降解剂，又是一种选择性的 BET BRD4 降解剂，FKBP12 PROTAC dTAG-7 (dTAG-7) 通过将 BET 溴结构域桥接至 E3 泛素连接酶 (cereblon; CRBN) 而形成降解剂。

  • GC39407 structure
    GC39407MS1943
    CAS: 2225938-17-8
    纯度: >98.00%

    A PROTAC that drives EZH2 degradation

  • GC39426 structure
    GC39426PROTAC SGK3 degrader-1
    CAS: 2381320-35-8
    纯度: >99.00%

    PROTAC SGK3 degrader-1 (SGK3-PROTAC1) is a PROTAC conjugate of the 308-R SGK inhibitor with the VH032 VHL binding ligand, targeting SGK3 (Serum/Glucocorticoid Regulated Kinase Family Member 3) for degradation.

  • GC39503 structure
    GC39503PROTAC FKBP Degrader-3
    CAS: 2079056-43-0
    纯度: >98.00%

    PROTAC FKBP Degrader-3 是一种包含 FKBP 配体结合基团，linker 和 VHL 结合基团的 PROTAC。PROTAC FKBP Degrader-3 是一种有效的 FKBP 降解剂。

  • GC39708 structure
    GC39708DT2216
    CAS: 2365172-42-3

    DT2216 是一种蛋白水解靶向嵌合体 (PROTAC)，靶向 Bcl-xL 降解依赖于 Bcl-2 家族过表达蛋白（例如 Bcl-2、Bcl-xL 和 Mcl）的 T 细胞淋巴瘤-1.DT2216 抑制 G-68 细胞，IC50 值为 4.02 μM（72 小时）。

  • GC40877 structure
    GC40877Heclin
    CAS: 890605-54-6
    纯度: >98.00%

    An inhibitor of HECT E3 ubiquitin ligases

  • GC48410 structure
    GC48410VH 032 Linker 3 (hydrate)
    纯度: >95.00%

    A VHL ligand 1 derivative

  • GC49728 structure
    GC49728PROTAC(H-PGDS)-7
    CAS: 2761281-50-7
    纯度: >95.00%

    PROTAC(H-PGDS)-7 是一种造血前列腺素 D 合酶 (H-PGDS) PROTAC 降解剂，DC50 为 17.3 pM。

  • GC50363 structure
    GC50363cis MZ 1
    CAS: 1797406-72-4

    Negative Control for MZ 1

  • GC50460 structure
    GC50460VH 032 amide-PEG3-amine
    CAS: 2376990-24-6

    VHL ligand with PEG linker and terminal amine for onward chemistry

  • GC50461 structure
    GC50461VH 032 amide-alkylC4-amine
    CAS: 2341796-78-7

    VH 032 酰胺-烷基C4-胺是一种合成的 E3 连接酶配体-接头偶联物，它包含基于 (S,R,S)-AHPC 的 VHL 配体和用于 EED-Targeted PROTAC 的接头。

  • GC50462 structure
    GC50462Thalidomide 4'-oxyacetamide-PEG3-amine
    CAS: 2245697-84-9
    纯度: >98.00%

    Thalidomide 4'-oxyacetamide-PEG3-amine 是一种合成的 E3 连接酶配体-接头偶联物，它包含用于 PROTAC 技术的基于 Thalidomide 的 cereblon 配体和 3 单元 PEG 接头。

  • GC50464 structure
    GC50464Thalidomide 4'-oxyacetamide-alkylC4-amine
    CAS: 2245697-86-1
    纯度: >98.00%

    Thalidomide 4'-oxyetamide-alkylC4-amine 是一种合成的 E3 连接酶配体-接头偶联物，包含基于 Thalidomide 的 cereblon 配体和接头，可用于 PROTAC 的合成。

  • GC50467 structure
    GC50467A 410099.1 amide-PEG3-amine
    CAS: 2415256-19-6

    A 410099.1 amide-PEG3-amine

  • GC50468 structure
    GC50468A 410099.1 amide-PEG2-amine
    CAS: 2415256-16-3

    A 410099.1 amide-PEG2-amine

  • GC50469 structure
    GC50469A 410099.1 amide-alkylC4-amine
    CAS: 2415256-18-5

    A 410099.1 amide-alkylC4-amine

  • GC50484 structure
    GC50484TL 12-186
    CAS: 2250025-88-6
    纯度: >98.00%

    TL 12-186 是一种依赖于大脑的多激酶 PROTAC 降解剂。多激酶包括 CDK、BTK、FLT3、Aurora 激酶、TEC、ULK、ITK 等。 TL 12-186 抑制 CDK2/cyclin A (IC50\u003d73 nM) 和 CDK9/cyclin T1 (IC50\u003d55 nM)。

  • GC50485 structure
    GC50485TL 13-27
    CAS: 2250025-90-0

    TL 12-186 的阴性对照

  • GC50518 structure
    GC50518dBRD9
    CAS: 2341840-98-8

    有效且选择性的 BRD9 降解 PROTAC

  • GC50530 structure
    GC50530Pomalidomide 4'-PEG2-amine
    CAS: 2245697-87-2

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

  • GC50543 structure
    GC50543VH 032 amide-PEG3-acid
    CAS: 2140807-42-5

    VH 032 amide-PEG3-acid 是一种合成的 E3 连接酶配体-接头偶联物，包含基于 (S,R,S)-AHPC 的 VHL 配体和用于 PROTAC 技术的 3 单元 PEG 接头。

  • GC50544 structure
    GC50544VH 032 amide-alkylC4-acid
    CAS: 2172819-74-6

    VHL ligand with alkyl linker and terminal acid for onward chemistry

  • GC50546 structure
    GC50546Pomalidomide 4'-alkylC5-acid
    CAS: 2225940-49-6
    纯度: >98.50%

    Pomalidomide 4'-alkylC5-acid 是一种合成的 E3 连接酶配体-接头偶联物，包含基于 Pomalidomide 的 cereblon 配体和 PROTAC 技术中使用的 PEG 接头。