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Home >> Signaling Pathways >> PROTAC >> 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.

Products for  PROTAC

  1. Cat.No. 产品名称 Information
  2. GC60307 PROTAC RIPK degrader-2 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。
  3. GC61215 PROTAC RIPK degrader-6 PROTACRIPKdegrader-6(example1)是一种PROTAC类的有效RIPK降解剂。
  4. GC39426 PROTAC SGK3 degrader-1

    SGK3-PROTAC1

     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.
  5. GC33418 PROTAC Sirt2 Degrader-1 PROTACSirt2Degrader-1是一种基于SirReal的PROTAC，为Sirt2的降解剂，由一个高效、同种型选择性的Sirt2抑制剂，一个连接物和thalidomide(E3泛素化连接酶的配体)组成。PROTACSirt2Degrader-1对Sirt2的IC50值为0.25μM，而对Sirt1/Sirt3(IC50>100μM)无作用
  6. GC33217 QCA570 QCA570是基于PROTAC技术的BET的强效降解剂，其对BRD4BD1蛋白的IC50值为10nM。
  7. GC50752 SJF 1521 Selective EGFR Degrader
  8. GC50748 SJF 1528 Potent EGFR Degrader (DC50 values are 39
  9. GC50753 SJF 8240 c-MET degrader
  10. GC33229 SJFα SJFα是一种含13个原子连接桥的PROTAC。SJFα降解p38α，DC50为7.16nM，但降解p38δ效果较差(DC50=299nM)，且在浓度高达2.5μM时也不会降解其他p38亚型(β和γ)。
  11. GC33238 SJFδ SJFδ是一种含10个原子连接桥的PROTAC。SJFδ降解p38α，DC50为46.17nM，但不降解其他p38亚型(p38α,p38β和p38γ)。
  12. GC50746 TBK1 control PROTAC® 4 Negative control for TBK1 PROTAC? 3i
  13. GC50745 TBK1 PROTAC® 3i Potent TANK-binding kinase 1 (TBK1) Degrader (DC50 = 12 nM, Dmax = 96%)
  14. GC34319 TD-428 TD-428是一种高度特异的BRD4降解剂，DC50为0.32nM。
  15. GC50608 Thalidomide 4'-ether-alkylC4-amine Cereblon ligand with alkyl linker and terminal amine for onward chemistry
  16. GC50621 Thalidomide 4'-ether-PEG3-amine Cereblon ligand with PEG linker and terminal amine for onward chemistry
  17. GC50709 Thalidomide 4'-oxyacetamide-alkylC1-PEG3-alkylC3-amine

    沙利度胺4'-氧乙酰胺-烷基C1-三聚乙二醇-烷基C3-氨基盐酸盐

     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
  18. GC50464 Thalidomide 4'-oxyacetamide-alkylC4-amine 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。
  19. GC50628 Thalidomide 4'-oxyacetamide-alkylC6-amine Thalidomide 4'-oxyetamide-alkylC6-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。
  20. GC50618 Thalidomide 4'-oxyacetamide-alkylC8-amine Cereblon ligand with alkyl linker and terminal amine for onward chemistry
  21. GC50627 Thalidomide 4'-oxyacetamide-PEG2-amine Thalidomide 4'-oxyacetamide-PEG2-amine 包含一个 E3 连接酶配体和一个接头，可以作为治疗癌症的免疫调节剂。
  22. GC50462 Thalidomide 4'-oxyacetamide-PEG3-amine

    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。
  23. GC50484 TL 12-186 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)。
  24. GC50561 TL 13-112 TL 13-112 是一种有效的选择性 ALK-PROTAC 降解剂，抑制 ALK 活性，IC50 值为 0.14 nM。 TL 13-112 还促进其他激酶的降解，包括 Aurora A、FER、PTK2 和 RPS6KA1，IC50 值分别为 8550 nM、42.4 nM、25.4 nM 和 677 nM。 TL 13-112 由色瑞替尼和 Pomalidomide 的 Cereblon 配体的结合物组成。
  25. GC50560 TL 13-12 TL 13-12 是一种有效的选择性 ALK-PROTAC 降解剂，可抑制 ALK 活性，IC50 值为 0.69 nM。 TL 13-12 还促进其他激酶的降解，包括 Aurora A、FER、PTK2 和 RPS6KA1，IC50 值分别为 13.5 nM、5.74 nM、18.4 nM 和 65 nM。 TL 13-12 由 TAE684 和 Pomalidomide 的 Cereblon 配体的缀合组成。
  26. GC50485 TL 13-27 TL 12-186 的阴性对照
  27. GC50712 VH 032 amide-alkylC2-acid 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
  28. GC50718 VH 032 amide-alkylC3-acid

    (S,R,S)-AHPC-CO-C3-酸

     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
  29. GC50714 VH 032 amide-alkylC3-amine 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
  30. GC50544 VH 032 amide-alkylC4-acid VHL ligand with alkyl linker and terminal acid for onward chemistry
  31. GC50461 VH 032 amide-alkylC4-amine

    VH032-C4-NH2 dihydrochloride

     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。
  32. GC50634 VH 032 amide-alkylC5-amine VHL ligand with alkyl linker and terminal amine for onward chemistry
  33. GC50724 VH 032 amide-alkylC6-acid 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
  34. GC50646 VH 032 amide-alkylC7-amine VHL ligand with alkyl linker and terminal amine for onward chemistry
  35. GC50730 VH 032 amide-alkylC8-acid 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
  36. GC50597 VH 032 amide-alkylC8-amine

    VH032-C8-NH2 dihydrochloride

     VH 032 amide-alkylC8-amine (VH032-C8-NH2 dihydrochloride) 是一种合成的 E3 连接酶配体-接头偶联物，它包含基于 VH032 的 VHL 配体和用于 AKTPROTAC 降解剂的接头。
  37. GC50720 VH 032 amide-PEG1-acid 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
  38. GC50591 VH 032 amide-PEG1-amine

    VH032-PEG1-NH2 dihydrochloride

     (S,R,S)-AHPC-PEG1-NH2 (VH032-PEG1-NH2) dihydrochloride 包含 E3 泛素连接酶的 VHL 配体和 PROTAC 接头。 VH 032 amide-PEG1-amine 可用于设计 PROTAC。
  39. GC50604 VH 032 amide-PEG2-amine

    VH032-PEG2-NH2 dihydrochloride

     VH 032 amide-PEG2-amine (VH032-PEG2-NH2 dihydrochloride) 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 2 单元 PEG 接头，用于合成PROTAC。
  40. GC50543 VH 032 amide-PEG3-acid 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。
  41. GC50460 VH 032 amide-PEG3-amine VHL ligand with PEG linker and terminal amine for onward chemistry
  42. GC50731 VH 032 amide-PEG4-amine 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
  43. GC50605 VH 032 phenol-alkylC4-amine

    VH032-phenol-C4-NH2 dihydrochloride

     (S,R,S)-AHPC-phenol-C4-NH2 (VH032-phenol-C4-NH2) dihydrochloride 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PROTAC技术中使用的链接器。
  44. GC50606 VH 032 phenol-alkylC6-amine

    VH032 phenol-alkylC6-amine dihydrochloride

     VH 032 苯酚-烷基C6-胺是一种合成的E3 连接酶配体-接头偶联物，它包含基于VH032 的VHL 配体和用于PROTAC 降解剂的烷基接头。
  45. GC50698 VH 032, amine 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
  46. GC50607 VH 032, phenol VH 032，苯酚是基于 VH032 的 VHL 配体。 VH 032，苯酚可以通过接头连接到蛋白质的配体上，形成PROTAC。
  47. GC50723 VH 101 phenol-alkylC4-amine 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
  48. GC50729 VH 101 phenol-alkylC6-amine 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
  49. GC50652 xStAx-VHLL Selective peptide-based β-catenin Degrader

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