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)

  • 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。

  • GC61481 structure
    GC61481PROTAC AR Degrader-4 TFA
    纯度: >98.00%

    PROTACARDegrader-4包含cIAP1配体结合基团，linker和雄激素受体(AR)配体结合基团。基于cIAP1的降解剂也被称为SNIPER。

  • GC61766 structure
    GC61766LC-2
    CAS: 2502156-03-6
    纯度: >95.00%

    LC-2 is a first PROTAC capable of degrading endogenous KRASG12C with DC50s between 0.25 μM and 0.76 μM. LC-2 covalently binds KRASG12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRASG12C degradation leading to suppression of MAPK signaling.

  • GC62942 structure
    GC62942DP-C-4
    纯度: >99.50%

    DP-C-4 是一种基于 Cereblon 的双 PROTAC，用于同时降解 EGFR 和 PARP。

  • GC63445 structure
    GC63445dBET23
    CAS: 1957234-83-1
    纯度: >99.00%

    dBET23 是一种高效、选择性的 PROTAC BRD4 降解剂，对 BRD4BD1 蛋白的 DC50/5h 约为 50 nM。

  • GC63492 structure
    GC63492ARD-2128
    CAS: 2222111-87-5

    ARD-2128 是一种高效的 PROTAC 雄激素受体 (AR) 降解剂。ARD-2128 可有效降低 AR 蛋白并抑制肿瘤组织中 AR 调节的基因，在没有毒性迹象的情况下抑制肿瘤生长。ARD-2128 作用在前列腺癌的研究上。