Beta Amyloid
信号通路图
研究领域
抑制剂选择性比较
Beta Amyloid产品
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2215 |
DAPT (GSI-IX)DAPT (GSI-IX, LY-374973) 是一种新型γ-secretase抑制剂，抑制 Aβ产生，在HEK 293细胞中IC50为20 nM。DAPT可促进人类舌癌细胞的凋亡并调节自噬。 |
Western blotting showing increased unconjugated SUMO1 levels in Notch1 ΔE cells treated with 10 uM DAPT for 3 days. Tubulin was used as a loading control.
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| S1575 |
RO4929097RO4929097 (RG-4733)是一种γ secretase抑制剂，无细胞试验中IC50为4 nM，抑制Aβ40和Notch的细胞加工，EC50分别为14 nM和5 nM。Phase 2。 |
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| S1594 |
Semagacestat (LY450139)Semagacestat (LY450139)是一种γ-分泌酶抑制剂，作用于Aβ42，Aβ40和Aβ38，IC50分别为10.9 nM，12.1 nM和12.0 nM，也抑制Notch信号通路，人神经胶质瘤细胞中IC50为14.1 nM。Phase 3。 |
HEK/APPswe cells were either left non-treated (-) or exposed to the γ-secretase inhibitor (GSI) semagacestat (+) for 19 h prior to cell harvesting and membrane preparation (Substrate accumulation). Exposure of cells with GSI prior to membrane preparation results in higher Aβ1-42 and Aβx-42 signals as compared to membranes derived from non-GSI treated cells. Direct addition of semagacestat to the membranes in the novo Aβ production assay inhibited Aβ production (Semagacestat (1 µM)). The amount of Aβx-42 is higher than Aβ1-42 suggesting that C83 is the major substrate for the Aβ42 signal detected. |
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| S2660 |
MK-0752MK-0752是一种适度有效的γ-secretase（γ-分泌酶）抑制剂，降低Aβ40产量，IC50为5 nM。Phase 1/2。 |
HES1 expression after treatment with clinically available GSIs R04929097, BMS-708163, LY450139, and MK-0752 as determined by qRT-PCR.
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| S1262 |
Avagacestat (BMS-708163)Avagacestat (BMS-708163)是口服生物有效的，选择性的γ-分泌酶抑制剂，作用于Aβ40和Aβ42时，IC50分别为0.3 nM和0.27 nM，比作用于Notch选择性高193倍。Phase 2。 |
A panel of GICs lines was treated with various concentrations of γ secretase inhibitors BMS-708163. Cells were treated with increasing concentrations of γ secretase inhibitors in triplicate wells for 72 hours, and cell viability was assessed by CellTiter-Blue assay as described in Materials and Methods. The results shown are of a single experiment with three independent replicates cell viability was measured by CellTiter-Blue assay. The graph depicts cell viability at 72 hours. Cell viability in the vehicle control was considered as to be 100%. |
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| S1528 |
LY2811376LY2811376是第一个口服有效的，非肽类β-secretase(BACE1)抑制剂，IC50为239 nM-249 nM，可以减少Aβ分泌，EC50为300 nM，作用于BACE1比作用于BACE2选择性高10倍，比作用于其他天冬氨酸蛋白酶（包括Cathepsin D，胃蛋白酶和肾素）抑制效果高50倍以上。Phase 1。 |
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| S0529 |
PBD-150PBD-150 是一种有效的人谷氨酰胺酰环化酶 (human glutaminyl cyclase，hQC) Y115E-Y117E 变异抑制剂，Ki 为 60 nM。 |
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| S4261 |
EUK 134EUK 134是一种合成的超氧化物歧化酶（SOD）/过氧化氢酶类似物，具有强效的抗氧化活性，且抑制β-amyloid（β-淀粉样蛋白）和相关的淀粉样纤维形成。 |
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| S4760 |
(2-Hydroxypropyl)-β-cyclodextrin (HP-β-CD)(2-Hydroxypropyl)-β-cyclodextrin (HP-β-CD, HP-β-cyclodextrin, Hydroxypropyl betadex, Hydroxypropyl-β-cyclodextrin), a well-known sugar used in drug delivery, genetic vector, environmental protection and treatment of Niemann-Pick disease type C1 (NPC1), is an inhibitor of amyloid-β aggregation. |
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| S8185 |
FPS-ZM1FPS-ZM1是一种能透过血脑障壁、无毒性、三级酰胺化合物。是RAGE的特异性抑制剂，抑制Aβ与RAGE的V区域结合。 |
FPS-ZM1 suppresses S100B promoted migration and invasion abilities. *P < 0.05, **P < 0.01 vs “CM” groups; &P < 0.05, &&P < 0.01 vs “S100B+FPS” groups. |
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| S5101 |
Tabersonine hydrochlorideTabersonine, an ingredient extracted from the bean of Voacanga africana, is a potent inhibitor against Aβ(1−42) aggregation and toxicity. |
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| S9664 |
ColivelinColivelin (CLN) 是一种脑渗透性的神经保护肽，对神经退行性疾病中的 Aβ 沉积，神经元凋亡和突触可塑性缺陷具有有效的长期作用。 Colivelin 是一种 STAT3 的激活剂。 |
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| S9087 |
TenuifolinTenuifolin, a secondary saponin isolated from hydrolysates of polygalasaponins, inhibits beta-amyloid synthesis in vitro and has nootropic activity in vivo via acetylcholine esterase inhibition and increases norepinephrine and dopamine production. |
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| S6733 |
Edonerpic maleateEdonerpic maleate (T-817)是一种神经营养性因子，可抑制amyloid-β peptides (Aβ)。 |
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| S3811 |
Ginsenoside ReGinsenoside Re (Ginsenoside B2, Panaxoside Re, Sanchinoside Re, Chikusetsusaponin Ivc)是三七的提取物、人参中的主要人参皂苷，属于20(S)-原人参三醇组 (protopanaxatriol group)。它具有多种体外和体内作用，包括血管舒张作用，抗氧化剂，抗高血脂和血管生成作用。Ginsenoside Re 会降低 β-amyloid protein (Aβ) 并通过抑制 JNK 和 NF-κB 起到抗炎的作用。 |
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| S2418 |
FrentizoleFrentizole (Frentizol)是一种新型 amyloid beta peptide (Abeta) 结合 alcohol dehydrogenase (ABAD) 相互作用的抑制剂，IC50为200μM。Frentizole是一种无毒的抗病毒和免疫抑制剂，临床上用于类风湿关节炎和系统性红斑狼疮。 |
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| S5742 |
Deferoxamine mesylate (Ba 33112)Deferoxamine mesylate (Ba 33112, Desferrioxamine B, DFOM, NSC 644468)是Deferoxamine的甲磺酸盐，它可形成铁络合物并用作螯合剂。Deferoxamine 是一种铁死亡的抑制剂，可在体外低氧和高血糖状态下稳定 HIF-1α 的表达并改善HIF-1α的活性。Deferoxamine 可降低 beta-amyloid (Aβ) 的沉积并诱导自噬。 |
||
| S3923 |
Ginsenoside Rg1Ginsenoside Rg1 (Ginsenoside A2, Panaxoside A, Panaxoside Rg1, Sanchinoside C1, Sanchinoside Rg1)是人参的主要活性成分之一，被确定为原人参三醇型，对多种癌症具有药理作用，例如神经保护和抗肿瘤作用。Ginsenoside Rg1 可降低 cerebral Aβ 水平并减少 NF-κB 核转移。 |
||
| S0486 |
Hoechst 34580Hoechst 34580 (HOE 34580) 是一种具有细胞渗透性的蓝色荧光染料，用于染色DNA和细胞核。Hoechst 34580 也是一种治疗阿尔茨海默病的良好候选者，通过抑制 amyloid beta (Aβ) 的形成，其IC50值为0.86 μM。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2215 |
DAPT (GSI-IX)DAPT (GSI-IX, LY-374973) 是一种新型γ-secretase抑制剂，抑制 Aβ产生，在HEK 293细胞中IC50为20 nM。DAPT可促进人类舌癌细胞的凋亡并调节自噬。 |
Western blotting showing increased unconjugated SUMO1 levels in Notch1 ΔE cells treated with 10 uM DAPT for 3 days. Tubulin was used as a loading control.
|
|
| S1575 |
RO4929097RO4929097 (RG-4733)是一种γ secretase抑制剂，无细胞试验中IC50为4 nM，抑制Aβ40和Notch的细胞加工，EC50分别为14 nM和5 nM。Phase 2。 |
|
|
| S1594 |
Semagacestat (LY450139)Semagacestat (LY450139)是一种γ-分泌酶抑制剂，作用于Aβ42，Aβ40和Aβ38，IC50分别为10.9 nM，12.1 nM和12.0 nM，也抑制Notch信号通路，人神经胶质瘤细胞中IC50为14.1 nM。Phase 3。 |
HEK/APPswe cells were either left non-treated (-) or exposed to the γ-secretase inhibitor (GSI) semagacestat (+) for 19 h prior to cell harvesting and membrane preparation (Substrate accumulation). Exposure of cells with GSI prior to membrane preparation results in higher Aβ1-42 and Aβx-42 signals as compared to membranes derived from non-GSI treated cells. Direct addition of semagacestat to the membranes in the novo Aβ production assay inhibited Aβ production (Semagacestat (1 µM)). The amount of Aβx-42 is higher than Aβ1-42 suggesting that C83 is the major substrate for the Aβ42 signal detected. |
|
| S2660 |
MK-0752MK-0752是一种适度有效的γ-secretase（γ-分泌酶）抑制剂，降低Aβ40产量，IC50为5 nM。Phase 1/2。 |
HES1 expression after treatment with clinically available GSIs R04929097, BMS-708163, LY450139, and MK-0752 as determined by qRT-PCR.
|
|
| S1262 |
Avagacestat (BMS-708163)Avagacestat (BMS-708163)是口服生物有效的，选择性的γ-分泌酶抑制剂，作用于Aβ40和Aβ42时，IC50分别为0.3 nM和0.27 nM，比作用于Notch选择性高193倍。Phase 2。 |
A panel of GICs lines was treated with various concentrations of γ secretase inhibitors BMS-708163. Cells were treated with increasing concentrations of γ secretase inhibitors in triplicate wells for 72 hours, and cell viability was assessed by CellTiter-Blue assay as described in Materials and Methods. The results shown are of a single experiment with three independent replicates cell viability was measured by CellTiter-Blue assay. The graph depicts cell viability at 72 hours. Cell viability in the vehicle control was considered as to be 100%. |
|
| S1528 |
LY2811376LY2811376是第一个口服有效的，非肽类β-secretase(BACE1)抑制剂，IC50为239 nM-249 nM，可以减少Aβ分泌，EC50为300 nM，作用于BACE1比作用于BACE2选择性高10倍，比作用于其他天冬氨酸蛋白酶（包括Cathepsin D，胃蛋白酶和肾素）抑制效果高50倍以上。Phase 1。 |
|
|
| S0529 |
PBD-150PBD-150 是一种有效的人谷氨酰胺酰环化酶 (human glutaminyl cyclase，hQC) Y115E-Y117E 变异抑制剂，Ki 为 60 nM。 |
||
| S4261 |
EUK 134EUK 134是一种合成的超氧化物歧化酶（SOD）/过氧化氢酶类似物，具有强效的抗氧化活性，且抑制β-amyloid（β-淀粉样蛋白）和相关的淀粉样纤维形成。 |
||
| S4760 |
(2-Hydroxypropyl)-β-cyclodextrin (HP-β-CD)(2-Hydroxypropyl)-β-cyclodextrin (HP-β-CD, HP-β-cyclodextrin, Hydroxypropyl betadex, Hydroxypropyl-β-cyclodextrin), a well-known sugar used in drug delivery, genetic vector, environmental protection and treatment of Niemann-Pick disease type C1 (NPC1), is an inhibitor of amyloid-β aggregation. |
||
| S8185 |
FPS-ZM1FPS-ZM1是一种能透过血脑障壁、无毒性、三级酰胺化合物。是RAGE的特异性抑制剂，抑制Aβ与RAGE的V区域结合。 |
FPS-ZM1 suppresses S100B promoted migration and invasion abilities. *P < 0.05, **P < 0.01 vs “CM” groups; &P < 0.05, &&P < 0.01 vs “S100B+FPS” groups. |
|
| S5101 |
Tabersonine hydrochlorideTabersonine, an ingredient extracted from the bean of Voacanga africana, is a potent inhibitor against Aβ(1−42) aggregation and toxicity. |
||
| S9664 |
ColivelinColivelin (CLN) 是一种脑渗透性的神经保护肽，对神经退行性疾病中的 Aβ 沉积，神经元凋亡和突触可塑性缺陷具有有效的长期作用。 Colivelin 是一种 STAT3 的激活剂。 |
||
| S9087 |
TenuifolinTenuifolin, a secondary saponin isolated from hydrolysates of polygalasaponins, inhibits beta-amyloid synthesis in vitro and has nootropic activity in vivo via acetylcholine esterase inhibition and increases norepinephrine and dopamine production. |
||
| S6733 |
Edonerpic maleateEdonerpic maleate (T-817)是一种神经营养性因子，可抑制amyloid-β peptides (Aβ)。 |
||
| S3811 |
Ginsenoside ReGinsenoside Re (Ginsenoside B2, Panaxoside Re, Sanchinoside Re, Chikusetsusaponin Ivc)是三七的提取物、人参中的主要人参皂苷，属于20(S)-原人参三醇组 (protopanaxatriol group)。它具有多种体外和体内作用，包括血管舒张作用，抗氧化剂，抗高血脂和血管生成作用。Ginsenoside Re 会降低 β-amyloid protein (Aβ) 并通过抑制 JNK 和 NF-κB 起到抗炎的作用。 |
||
| S2418 |
FrentizoleFrentizole (Frentizol)是一种新型 amyloid beta peptide (Abeta) 结合 alcohol dehydrogenase (ABAD) 相互作用的抑制剂，IC50为200μM。Frentizole是一种无毒的抗病毒和免疫抑制剂，临床上用于类风湿关节炎和系统性红斑狼疮。 |
||
| S5742 |
Deferoxamine mesylate (Ba 33112)Deferoxamine mesylate (Ba 33112, Desferrioxamine B, DFOM, NSC 644468)是Deferoxamine的甲磺酸盐，它可形成铁络合物并用作螯合剂。Deferoxamine 是一种铁死亡的抑制剂，可在体外低氧和高血糖状态下稳定 HIF-1α 的表达并改善HIF-1α的活性。Deferoxamine 可降低 beta-amyloid (Aβ) 的沉积并诱导自噬。 |
||
| S3923 |
Ginsenoside Rg1Ginsenoside Rg1 (Ginsenoside A2, Panaxoside A, Panaxoside Rg1, Sanchinoside C1, Sanchinoside Rg1)是人参的主要活性成分之一，被确定为原人参三醇型，对多种癌症具有药理作用，例如神经保护和抗肿瘤作用。Ginsenoside Rg1 可降低 cerebral Aβ 水平并减少 NF-κB 核转移。 |
||
| S0486 |
Hoechst 34580Hoechst 34580 (HOE 34580) 是一种具有细胞渗透性的蓝色荧光染料，用于染色DNA和细胞核。Hoechst 34580 也是一种治疗阿尔茨海默病的良好候选者，通过抑制 amyloid beta (Aβ) 的形成，其IC50值为0.86 μM。 |
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