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Gamma Secretase(伽玛分泌酶)

Gamma secretase (γ-secretase), a member of the intramembrane cleaving protease (i-CLiP) family, is a promiscuous di-aspartyl protease that catalyzes the regulated intramembrane proteolysis (RIP), in which substrate proteins are cleaved within their membrane-spanning domain. A functional γ-secretase is a multi-protein complex consisting of the catalytic component, presenilin (PSEN), and three protein cofactors, including nicastrin (NCT), anterior-pharynx defective-1 (APH1) and PSEN enhancer-2 (PEN2). So far, 90 substrates of γ-secretase have been identified, which are type-I transmembrane proteins, except for glutamate receptor GluR3, polycystin-1 and glucosaminyltransferase (GnT-V), and appear to function as signaling proteins regulating a wide variety of cellular events, such as Notch signaling pathway.

Products for  Gamma Secretase

  1. Cat.No. 产品名称 Information
  2. GC67476 (E/Z)-Sulindac sulfide (E/Z)-Sulindac sulfide 是一种有效的 γ-secretase 调节剂。(E/Z)-Sulindac sulfide 可选择性地减少 Aβ42 产生,有利于更短的 Aβ 类型的产生。(E/Z)-Sulindac sulfide 可用于阿尔兹海默症的研究。
  3. GC63407 PF-06648671 PF-06648671 是一种新型的,可通透血脑屏障的,具有口服活性的 γ 分泌酶 (γ‐Secretase) 调节剂 (GSM)。PF-06648671 减少 Aβ42 和 Aβ40,并且伴随 Aβ37 和 Aβ38 的增加。PF-06648671 用于阿尔茨海默病的研究。
  4. GC63366 Fosciclopirox Fosciclopirox(CPX-POM) selectively delivers the active metabolite, Ciclopirox (CPX) that targets γ-secretase complex (Presenilin 1 and Nicastrin)2. It is used in the treatment of urothelial cancer and a number of solid and hematologic malignancies.
  5. GC62998 GSM-1 GSM-1 是有效的 γ-secretase 调节剂。GSM-1 直接靶向早衰蛋白 1 (PS1) 的跨膜结构域。
  6. GC62859 Aβ42-IN-2 Aβ42-IN-2 是一种 γ-secretase 调节剂,详细信息请参考专利文献 WO2016070107 中 的化合物 36。Aβ42-IN-2 对 αβ42 作用的 IC50 值为 6.5 nM 。Aβ42-IN-2 可用于阿尔茨海默症的研究。
  7. GC50251 PF 3084014 hydrobromide An inhibitor of γ-secretase
  8. GC38782 gamma-secretase modulator 1 hydrochloride gamma-secretase inhibitior-1 是 γ-secretase 调节剂,可作用于阿尔茨海默病。
  9. GC38011 γ-Secretase modulator 4 γ-Secretase modulator 4 是一种有效的 γ- 分泌酶调节剂 (γ-secretase),在人类和小鼠中降低 Aβ42 产生的 IC50 值分别为 0.014 μM 和 0.017 μM。
  10. GC36514 LY-411575 isomer 3 LY-411575 isomer 3 是 LY411575 的一个异构体,LY411575 为 γ-secretase 高效抑制剂。
  11. GC36513 LY-411575 isomer 2 LY-411575 isomer 2 是 LY411575 的一个异构体,LY411575 为 γ-secretase 高效抑制剂。
  12. GC36512 LY-411575 isomer 1 LY-411575 isomer 1 是 LY411575的一个异构体,LY411575为γ-secretase 高效抑制剂。
  13. GC36109 gamma-secretase modulator 3 gamma-secretase modulator 3是γ-secretase调节剂。
  14. GC36108 gamma-secretase modulator 2 Gamma-secretase modulator 2是γ-secretase调节剂,可用于阿尔兹海默。
  15. GC36107 gamma-secretase modulator 1 γ-secretase inhibitior-1是γ-secretase调节剂,可作用于阿尔茨海默病。
  16. GC35921 E 2012 A γ-secretase modulator
  17. GC35535 BMS-906024 BMS-906024 是一种口服有效,选择性的 γ 分泌酶 (gamma secretase) 抑制剂 (GSI),GSIs 是一类小分子 Notch 抑制剂。BMS-906024 可阻止具有高口服生物利用度的所有四种 Notch 受体的激活,对于 Notch1,-2,-3 和 -4 受体,IC50s 分别为 1.6,0.7,3.4 和 2.9 nM。 BMS-906024 表现出针对多种人癌症异种移植物的广谱抗肿瘤活性。
  18. GC33118 Compound E An inhibitor of γ-secretase
  19. GC31012 BMS 433796 BMS433796是一种γ-分泌酶抑制剂,用于阿尔茨海默氏病转基因小鼠模型,可降低Aβ活性。
  20. GC30954 Itanapraced (CHF5074) A modulator of γ-secretase
  21. GC30887 NGP555 A γ-secretase modulator
  22. GC30427 ELN 318463 racemate ELN318463racemate是ELN318463的外消旋体。ELN318463是一种选择性的gamma-secretase抑制剂。
  23. GC19290 PF-3084014 An inhibitor of γ-secretase
  24. GC15059 Sulindac sulfide An active metabolite of sulindac
  25. GC15896 Z-Ile-Leu-aldehyde Z-Ile-Leu-aldehyde (Z-IL-CHO) 是一种有效的、竞争性的 γ-分泌酶和缺口肽醛抑制剂。
  26. GC16434 TC-E 5006 γ-secretase modulator
  27. GC12659 Begacestat An inhibitor of γ-secretase
  28. GC10064 Flurizan A COX-inactive enantiomer of flurbiprofen
  29. GC16431 MRK 560 A potent inhibitor of γ-secretase
  30. GC15364 L-685,458 A γ-secretase inhibitor
  31. GC13619 JLK 6 A protease inhibitor
  32. GC15645 Compound W A Notch1 signaling modulator
  33. GC13099 BMS 299897 A γ-secretase inhibitor
  34. GC10998 PF-03084014

    γ-secretase inhibitor

  35. GC12653 LY3039478 A Notch inhibitor
  36. GC13673 BMS-708163 (Avagacestat) A potent inhibitor of γ-secretase
  37. GC17791 LY2811376 A BACE1 inhibitor
  38. GC12191 LY-411575 A γ-secretase inhibitor
  39. GC17671 YO-01027 (Dibenzazepine, DBZ) An inhibitor of γ-secretase
  40. GC15899 MK-0752 A potent inhibitor of γ-secretase
  41. GC16197 RO4929097

    An inhibitor of γ-secretase

  42. GC12942 DAPT (GSI-IX) Inhibitor of γ-secretase
  43. GC12096 Semagacestat (LY450139) A pan γ-secretase inhibitor

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