GlpBio

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)

  • 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

  • GC50739 structure
    GC50739A 410099.1 amide-PEG5-amine
    CAS: 2446474-11-7
    纯度: >95.00%

    Functionalized IAP ligand for PROTAC® research and development; incorporates an IAP ligand plus an amide-PEG5 linker with terminal amine ready for conjugation to a target protein ligand

  • GC50740 structure
    GC50740NR 7h
    CAS: 2550399-06-7
    纯度: >97.00%

    Potent and selective p38α and p38β degrader (DC50 < 50 nM)

  • GC50744 structure
    GC50744ARCC 4 negative control
    CAS: 2156588-26-8
    纯度: >98.00%

    Negative control for ARCC 4

  • GC50745 structure
    GC50745TBK1 PROTAC&#174; 3i
    CAS: 2052306-13-3
    纯度: >98.00%

    Potent TANK-binding kinase 1 (TBK1) Degrader (DC50 = 12 nM, Dmax = 96%)

  • GC50746 structure
    GC50746TBK1 control PROTAC&#174; 4
    CAS: 2052306-31-5
    纯度: >98.00%

    Negative control for TBK1 PROTAC? 3i

  • GC50748 structure
    GC50748SJF 1528
    CAS: 2230821-38-0
    纯度: >98.00%

    Potent EGFR Degrader (DC50 values are 39

  • GC50749 structure
    GC50749DD 03-171
    CAS: 2366132-45-6
    纯度: >98.00%

    Potent and selective BTK Degrader (IC50 = 5

  • GC50752 structure
    GC50752SJF 1521
    CAS: 2230821-40-4
    纯度: >98.00%

    Selective EGFR Degrader

  • GC50753 structure
    GC50753SJF 8240
    CAS: 2230821-68-6
    纯度: >98.00%

    c-MET degrader

  • GC50754 structure
    GC50754dTAG-13-NEG
    CAS: 2451573-90-1
    纯度: >98.00%

    Negative control for dTAG-13

  • GC50755 structure
    GC50755dTAGV-1-NEG
    CAS: 2451573-87-6
    纯度: >99.50%

    dTAGV-1-NEG 是一种非对映异构体，是 dTAGV-1 的异双功能阴性对照。 dTAGV-1 是一种 FKBP12F36V 选择性降解剂。

  • GC50756 structure
    GC50756dTAGV-1 TFA
    CAS: 2624313-15-9
    纯度: >98.00%

    Degrader targeting mutant FKBP12F36V fusion proteins

  • GC50757 structure
    GC50757dTAGV-1 hydrochloride
    CAS: 2624313-16-0
    纯度: >98.00%

    Hydrochloride salt of dTAGV-1

  • GC60009 structure
    GC60009(S,R,S)-AHPC-PEG5-COOH
    CAS: 2172820-14-1
    纯度: >95.00%

    (S,R,S)-AHPC-PEG5-COOH (VH032-PEG5-COOH) 是一种合成的 E3 连接酶配体-linker 偶联物，包含基于 (S,R,S)-AHPC 的 VHL 配体和 5 个单元 PEG linker。

  • GC60307 structure
    GC60307PROTAC RIPK degrader-2
    CAS: 1801547-16-9
    纯度: >99.00%

    PROTAC RIPK degrader-2 是一种非肽性PROTAC，它以丝氨酸苏氨酸激酶 RIPK2 为靶点，对 RIPK2 的降解具有高度选择性。

  • GC60594 structure
    GC60594ARCC-4
    CAS: 1973403-00-7
    纯度: >99.50%

    ARCC-4是基于PROTAC技术的，纳摩尔级的雄激素受体(AR)降解剂，其D50值为5 nM。ARCC-4是一种基于enzalutamide的vonHippel-Lindau(VHL)招募的ARPROTAC。ARCC-4能有效降解与抗雄激素研究相关的AR突变。

  • GC61200 structure
    GC61200Pomalidomide-PEG1-C2-N3
    CAS: 2271036-44-1
    纯度: >99.50%

    Pomalidomide-PEG1-C2-N3是一种合成的E3连接酶配体-linker偶联物，包含基于Pomalidomide的cereblon配体和1个单元PEG的linker。Pomalidomide-PEG1-C2-N3可通过PROTAC技术合成选择性的CDK6降解剂CP-10。CP-10诱导CDK6降解，DC50为2.1nM。

  • GC61212 structure
    GC61212PROTAC BRD4 Degrader-5
    CAS: 2409538-70-9
    纯度: >99.50%

    PROTACBRD4Degrader-5是一种基于PROTAC的BRD4降解剂，可有效降解HER2阳性和阴性乳腺癌细胞系中的BRD4。

  • GC61215 structure
    GC61215PROTAC RIPK degrader-6
    CAS: 2089205-64-9
    纯度: >99.00%

    PROTACRIPKdegrader-6(example1)是一种PROTAC类的有效RIPK降解剂。