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