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
- Cat.No. 产品名称 Information
- 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。
- 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。
- 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.
- 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。
- 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。
- GC50251 PF 3084014 hydrobromide An inhibitor of γ-secretase
- 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。
- 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。
- 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。
- 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。
- 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。
- GC36109 gamma-secretase modulator 3 gamma-secretase modulator 3是γ-secretase调节剂。
- GC36108 gamma-secretase modulator 2 Gamma-secretase modulator 2是γ-secretase调节剂,可用于阿尔兹海默。
- 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。
- GC35921 E 2012 A γ-secretase modulator
- 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。
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GC33118
Compound E
An inhibitor of γ-
secretase - 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。
- GC30954 Itanapraced (CHF5074) A modulator of γ-secretase
- GC30887 NGP555 A γ-secretase modulator
- 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。
- GC19290 PF-3084014 An inhibitor of γ-secretase
- GC15059 Sulindac sulfide An active metabolite of sulindac
- 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。
- GC16434 TC-E 5006 γ-secretase modulator
- GC12659 Begacestat An inhibitor of γ-secretase
- GC10064 Flurizan A COX-inactive enantiomer of flurbiprofen
- GC16431 MRK 560 A potent inhibitor of γ-secretase
- GC15364 L-685,458 A γ-secretase inhibitor
- GC13619 JLK 6 A protease inhibitor
- GC15645 Compound W A Notch1 signaling modulator
- GC13099 BMS 299897 A γ-secretase inhibitor
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GC10998
PF-03084014
γ-secretase inhibitor
- GC12653 LY3039478 A Notch inhibitor
- GC13673 BMS-708163 (Avagacestat) A potent inhibitor of γ-secretase
- GC17791 LY2811376 A BACE1 inhibitor
- GC12191 LY-411575 A γ-secretase inhibitor
- GC17671 YO-01027 (Dibenzazepine, DBZ) An inhibitor of γ-secretase
- GC15899 MK-0752 A potent inhibitor of γ-secretase
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GC16197
RO4929097
An inhibitor of γ-secretase
- GC12942 DAPT (GSI-IX) Inhibitor of γ-secretase
- GC12096 Semagacestat (LY450139) A pan γ-secretase inhibitor