43
9
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T9713 |
δ-secretase inhibitor 11
|
Beta Amyloid; Caspase | Apoptosis; Neuroscience; Proteases/Proteasome |
δ-secretase inhibitor 11是一种分泌酶抑制剂,可用作 阿尔茨海默病(AD) 治疗转化开发的先导化合物。 | |||
T40260 |
β-Secretase Inhibitor II
|
||
β-Secretase Inhibitor II is a tripeptide aldehyde compound that acts as an inhibitor of β-Secretase. It exhibits a simple structure and has an inhibitory potency of IC50 = 700 nM against total Aβ and IC50 = 2.5 μM specifically against Aβ 1-42. This compound is particularly useful in research related to Alzheimer's disease. | |||
T39251 |
β-Secretase Inhibitor I
|
||
β-Secretase Inhibitor I is a highly potent inhibitor of the β-secretase enzyme. This compound exhibits exceptional inhibitory activity while also demonstrating a significant reduction in cardiovascular and liver toxicity. | |||
T3161 |
β-Secretase inhibitor-STA
|
Beta-Secretase | Neuroscience |
BACE-IN-1 是淀粉样前体蛋白 β-分泌酶抑制剂。 | |||
T13434 |
β-Secretase Inhibitor IV
|
Others | Others |
β-Secretase Inhibitor IV is a potent, cell-active inhibitor of BACE-1(IC50s of 15.6 and 16.3nM under BACE-1 concentrations of 2 nM and 100 pM, respectively). | |||
T4398 |
LX2343
|
Beta Amyloid; Beta-Secretase; BACE; PI3K; Autophagy | Autophagy; Neuroscience; PI3K/Akt/mTOR signaling |
LX2343 是一种非 ATP 竞争性 PI3K 抑制剂,IC50 为 15.99±3.23 μM。它是一种 BACE1 酶抑制剂,IC50 值为 11.43±0.36 μM。它在促进 Aβ 清除中刺激自噬。 | |||
T12188 |
NB-360
|
BACE | Neuroscience |
NB-360 是一种有效的脑穿透性 BACE1 和 BACE2 抑制剂,对小鼠和人源 BACE1 和 BACE2 的 IC50 分别为 5、5 和 6 nM。 NB-360 对相关的天冬氨酰蛋白酶、胃蛋白酶、组织蛋白酶 E 和组织蛋白酶 D 具有出色的特异性。 | |||
T2639 |
LY2811376
|
Beta Amyloid; Beta-Secretase; BACE | Neuroscience |
LY2811376 是可口服的非肽段β-secretase (BACE1)抑制剂,IC50=239 nM-249 nM,能够降低 Aβ 蛋白的分泌,EC50=300 nM。 | |||
T13253 |
Umibecestat
CNP520 |
BACE | Neuroscience |
Umibecestat 是一种β-位点淀粉样前体蛋白裂解酶-1 (BACE-1) 抑制剂,对人 BACE-1 和小鼠 BACE-1 的 IC50 分别为 11 nM 和 10 nM,可用于阿尔茨海默病的研究。 | |||
T6125 |
Semagacestat
LY450139,塞美司他 |
Beta Amyloid; Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
Semagacestat (LY450139) 是一种γ-secretase 抑制剂,抑制β-amyloid(Aβ42),Aβ38和Aβ40,IC50分别为 10.9,12 和 12.1 nM,可用于研究阿尔茨海默病。 | |||
T6202 |
DAPT
LY-374973,GSI-IX |
Apoptosis; Beta Amyloid; Gamma-secretase; Autophagy | Apoptosis; Autophagy; Neuroscience; Proteases/Proteasome; Stem Cells |
DAPT (LY-374973) 是一种 γ 分泌酶抑制剂,抑制总 Aβ 和 Aβ42 (IC50=115/200 nM),具有口服活性。DAPT 也是一种 Notch 抑制剂。DAPT 可以诱导细胞分化、诱导细胞自噬和凋亡。 | |||
T6058 |
LY2886721
|
Beta-Secretase; BACE | Neuroscience |
LY2886721 是选择性的,口服活性的 β 位淀粉样蛋白前体蛋白裂解酶 1 抑制剂,对重组人 BACE1的 IC50=20.3 nM。它对 BACE1的选择性高于对组织蛋白酶 D、胃蛋白酶、肾素的选择性,但缺乏对 BACE2的选择性。它可透过血脑屏障,并可用于研究阿尔茨海默氏病。 | |||
T11175 |
Elenbecestat
E2609 |
Beta-Secretase; BACE | Neuroscience |
Elenbecestat (E2609) 是一种高效、有口服活性的,能透过 CNS 的 BACE-1抑制剂,它有用于阿尔茨海默病 (AD) 的研究潜力。 | |||
T6772 |
AZD3839 free base
AZD3839 |
Beta-Secretase; BACE | Neuroscience |
AZD3839 free base 是一种具有口服活性的、选择性的、可透过大脑屏障的BACE1抑制剂 (Ki=26 nM),对 BACE2 和组织蛋白酶 D 的选择性分别为 14 倍和 >1000 倍。在小鼠、豚鼠和非人灵长类动物中,它剂量和时间依赖性的降低血浆、脑和脑脊液 Aβ 水平,可用于研究阿尔茨海默病。 | |||
T7011 |
Verubecestat
MK-8931,维罗司他 |
Beta-Secretase; BACE | Neuroscience |
Verubecestat (MK-8931) 是一种高亲和力的、具有口服活性的BACE1和BACE2抑制剂,Ki 分别为 2.2 nM 和 0.38 nM。它可以有效降低 Aβ40,并具有潜力用于阿尔茨海默氏病。 | |||
T3285 |
Eslicarbazepine Acetate
Zebinix,Aptiom,BIA 2-093,Exalief,艾司利卡西平醋酸酯,Stedesa |
Beta-Secretase; Sodium Channel | Membrane transporter/Ion channel; Neuroscience |
Eslicarbazepine Acetate (Zebinix) 是一种抗癫痫药物。Eslicarbazepine acetate 也是 β-内分泌酶(β-Secretase)和电压门控钠离子通道的双抑制剂。 | |||
T11362 |
gamma-Secretase Modulators
γ-Secretase Modulators,Amyloid-β production inhibitor |
Others | Others |
gamma-Secretase Modulators serves as a useful treatment for Alzheimer's disease by inhibiting the production of Amyloid-β. Specifically, it acts as a gamma-Secretase Modulators with an IC50 value. | |||
T11358 |
gamma-secretase modulator 1
N-[3-methoxy-4-(4-methylimidazol-1-yl)phenyl]-4-phenyl-4,5,6,7-tetrahydro-1,3-benzothiazol-2-amine |
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
gamma-secretase modulator 1 是一种 γ 分泌酶的调节剂,可用于治疗阿尔茨海默病的研究。 | |||
T62455 | β-Secretase Inhibitor III | ||
β-Secretase Inhibitor III 是一种高度选择性的 BACE1 抑制剂,其 Ki 值为 0.13 nM。 | |||
T40315 | γ-Secretase modulator 10 | ||
γ-Secretase modulator 10 is a novel γ-secretase modulator. | |||
T61881 |
γ-Secretase modulator 12
|
||
γ-Secretase modulator 12 (Compound 1a) is a selective compound that effectively reduces amyloid-β42 (Aβ42) levels with an IC50 of 0.39 μM. It is specifically designed for Alzheimer's disease research. Notably, γ-Secretase modulator 12 exhibits a favorable brain/plasma ratio (Kp, brain = 0.72) in mice [1]. | |||
T63216 |
γ-Secretase modulator 11
|
||
5-{8-[(3,4'-二氟[1,1'-联苯]-4-基)甲氧基]-2-甲基咪唑并[1,2-a]吡啶-3-基}-N-甲基吡啶-2-甲酰胺(1o)具有较高的体外效力和脑暴露效果,能够使脑Aβ42水平的明显降低,且对细胞色素p450酶无抑制作用。此外,化合物1o 在AD 模型小鼠中表现出优异的抗认知缺陷作用。 | |||
T64258 | gamma-secretase modulator 5 | ||
gamma-secretase modulator 5 (compound 22d) 是一种能够透过血脑屏障的 γ-分泌酶调节剂 (GSMs),对聚集的淀粉样蛋白 β 肽 Aβ42 的产生表现出抑制作用 (IC50: 60 nM)。gamma-secretase modulator 5 能够用于研究阿尔茨海默病。 | |||
T63638 |
γ-Secretase modulator 11 hydrochloride
|
||
γ-Secretase modulator 11 hydrochloride 是有效的、口服具有活力的 γ-secretase 调节剂 (IC50: 0.029 μM)。 γ-Secretase modulator 11 hydrochloride 能够明显降低脑 Aβ42 水平,可挽救 AD 模型小鼠表现出的认知缺陷。γ-Secretase modulator 11 hydrochloride 对阿尔茨海默病表现出研究潜力。 | |||
T3521 |
γ-Secretase-IN-1
Compound E |
Beta Amyloid; Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
γ-Secretase-IN-1 是一种高效的 γ-secretase 抑制剂,对T-47D 细胞显示部分抗增殖活性且抑制 β-amyloid(40),β-amyloid(42),和Notch γ-分泌酶裂解。 | |||
T62263 |
γ-Secretase modulator 13
|
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
γ-Secretase modulator 13 是一种 γ-分泌酶调节剂 (GSMs),可以抑制淀粉样蛋白 β 肽Aβ42 的产生,可以用于研究阿尔茨海默病和肿瘤。 | |||
T11043 |
Dihydroergocristine mesylate
甲磺酸双氢麦角汀,DHEC (mesylate) |
Beta Amyloid | Neuroscience |
Dihydroergocristine mesylate (DHEC (mesylate)) 是一种 γ-secretase (GSI) 的抑制剂,能够阿尔茨海默氏病淀粉样蛋白 β 肽 (amyloid-β) 的产生,与 γ-secretase 和 Nicastrin 结合的平衡解离常数 (Kd) 值分别为 25.7 nM 和 9.8 μM。 | |||
T21890 |
JLK6
|
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
JLK-6 是一种γ分泌酶抑制剂,选择性作用于 HEK293细胞的淀粉样β前体蛋白(APP)的γ-分泌酶裂解 APP,抑制 Aβ的生成,但对不 Notch 受体的裂解无影响。 | |||
TP1786L |
Amyloid β-Protein 10-20 acetate
Amyloid β-Protein 10-20 acetate(152286-31-2 free base) |
Beta Amyloid | Neuroscience |
Amyloid β-Protein 10-20 acetate (Amyloid β-Protein 10-20 acetate (152286-31-2 free base)) 是 Amyloid-β 肽的片段,可能用于神经系统疾病的研究。Amyloid β 蛋白片段含有 α-分泌酶加工位点(Lys16-Leu17 键)。它还包含负责与小胶质细胞结合的 HHQK 结构域(残基 13-16)。 | |||
T4364 |
Aftin-4
Aftin 4,Aftin4 |
Beta Amyloid; Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
Aftin-4 是一种 β-淀粉样蛋白42(Aβ42) 的诱导剂。 | |||
T83616 |
SEW06622
|
BACE; AChE | Neuroscience |
SEW06622 是一种有效的 乙酰胆碱酯酶(AChE)和β-分泌酶-1(BACE-1)抑制剂,是治疗阿尔茨海默病的潜在候选化合物。 | |||
T15184 |
E 2012
(E)-1-[(1S)-1-(4-氟苯基)乙基]-3-[3-甲氧基-4-(4-甲基-1H-咪唑-1-YL)亚苄基]哌啶-2-酮 |
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
E 2012 是一种γ 分泌酶调节剂,不会影响 Notch 加工,在胆固醇生物合成的末步抑制 3β-羟基固醇 Δ24-还原酶。它能够减少淀粉样蛋白 β-42 减少阿兹海默氏病,并在大鼠多次重复给药后诱发白内障。 | |||
T6870 |
L-685458
L-685,458 |
Apoptosis; Gamma-secretase | Apoptosis; Neuroscience; Proteases/Proteasome; Stem Cells |
L-685458 (L-685,458) 是一种过渡状态模拟 γ-分泌酶抑制剂,抑制淀粉样 β-蛋白前体 γ-分泌酶活性,选择性高于其他检测的天冬氨酸蛋白酶 50-100 倍。它抑制 γ-分泌酶介导的 APP-C99 和 Notch-100 的裂解,可研究阿尔茨海默病和癌症。 | |||
T70366 | PF-06663195 | ||
PF-06663195 is a potent inhibitor of β-site amyloid precursor protein (APP) Cleaving Enzyme 1 (BACE1, β-Secretase 1). | |||
TP1099 |
M-2420
Methoxycoumarin-Ser-Glu-Val-Asn-Leu-Asp-Ala-Glu-Phe-Lys-dinitrophenyl |
||
M-2420 is a fluorogenic substrate designed specifically for the β-secretase site found in the Swedish mutation of the amyloid precursor protein (APP). | |||
TP1786 |
β-Amyloid (10-20)
Amyloid β-Protein 10-20 |
||
Amyloid β-Protein (10-20) is a fragment of Amyloid-β peptide, maybe used in the research of neurological disease.Amyloid β protein fragment containing the α-secretase processing site (Lys16-Leu17 bond). It also contains the HHQK domain (residues 13-16) re | |||
T25685 |
Leucyl-phenylalanine amide
Leu-phe-NH2 |
||
Leucyl-phenylalanine amide is an intermediate in the synthesis of γ-Secretase Inhibitor, the enzyme complex that catalyzes the cleavage of the amyloid precursor protein (APP) to produce amyloid β-peptide (Aβ) which is the major causative agent in Alzheime | |||
T39678 | Multitarget AD inhibitor-1 | ||
Multitarget AD inhibitor-1 is a reversible and selective inhibitor of butyrylcholinesterase (BuChE) with IC50 values of 7.22 μM and 1.55 μM for human BuChE (hBuChE) and equine serum BuChE (eqBuChE), respectively. Additionally, it exhibits inhibitory activity towards β-secretase (IC50 value of 41.60 μM), amyloid β aggregation (IC50 value of 3.09 μM), and tau aggregation. As a diphenylpropylamine derivative, Multitarget AD inhibitor-1 holds promise for research pertaining to the multifunctional, d... | |||
T63215 |
COX-2-IN-22
|
||
COX-2-IN-22 是一种能够透过血脑屏障的 COX-2 抑制剂 (IC50: 8.6 μM),也对AChE (IC50: 2.8 μM)、BChE (IC50: 6.3 μM)、β-Secretase (IC50: 15.3 μM)、LOX-5 (IC50: 13.9 μM) 和 DPPH (IC50: 6.8 μM)表现出抑制作用。 | |||
T37661 |
LY 2886721 Hydrochloride
|
||
Potent and selective β-secretase (BACE) inhibitor (IC50 values are 10.2 and 20.3 nM for human BACE2 and BACE1, respectively). Displays >5,000-fold selectivity for BACE over other proteases including cathepsin D, pepsin and renin. Inhibits Aβ1-40 and Aβ1-42 production in cells expressing mutated APP. Reduces hippocampal and cortical Aβ and sAPPβ levels in an Alzheimer's disease mouse model. | |||
T79422 |
BuChE-IN-8
|
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BuChE-IN-8 (compound 19c) 为有效抑制 BuChE 的化合物,IC50 值为 559 nM;展现对 BACE1 及 Aβ40 聚集的抑制活性,亦具有显著的抗遗忘特性。 | |||
T35975 |
6,9-Dichloro-1,2,3,4-tetrahydroacridine
|
||
6,9-Dichloro-1,2,3,4-tetrahydroacridine is a synthetic intermediate in the synthesis of tacrine-based acetylcholinesterase (AChE) inhibitors.1It is also an intermediate in the synthesis of multifunctional tacrine hybrids that possess radical scavenging, amyloid-β aggregation inhibitory, and/or β-secretase 1 (BACE1) inhibitory activities in addition to their activity as AChE inhibitors.2,3 1.Recanatini, M., Cavalli, A., Belluti, F., et al.SAR of 9-amino-1,2,3,4-tetrahydroacridine-based acetylchol... | |||
T83686 |
Mca-SEVNLDAEFR-K(Dnp)-RR-NH2 acetate
|
||
Mca-SEVNLDAEFR-K(Dnp)-RR-NH2是β-分泌酶(BACE)的荧光底物。当BACE切割该底物时,7-甲氧基香豆素-4-乙酰基(Mca)会被释放出来,其荧光可用于定量BACE活性。Mca的激发/发射最大值分别为328/420 nm。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T5S2361 |
Epiberberine
|
ERK; Beta-Secretase; MEK; BACE; AMPK; AChR; AChE | Chromatin/Epigenetic; MAPK; Neuroscience; PI3K/Akt/mTOR signaling |
Epiberberine 是一种从黄连中得到的生物碱,是AChE 和BChE 抑制剂,和非竞争性BACE1抑制剂。在 3T3-L1 细胞分化早期,它能够下调 Raf/MEK1/2/ERK1/2 和 AMPKα/Akt 信号通路。它具有抗氧化作用,能够清除 ONOO-,可用于阿尔滋海默症和糖尿病的研究。 | |||
T3769 |
Tenuifolin
|
Others; Beta-Secretase; AChE | Neuroscience; Others |
Tenuifolin 是一种从远志中分离出的三萜,能够抑制β-secretase 以减少 Aβ 蛋白分泌,具有神经保护作用。 它可通过降低 AChE 活性来改善衰老小鼠的学习和记忆能力,有潜力用于阿尔茨海默氏病的研究。 | |||
T8179 |
Aloeresin D
芦荟新甙D,芦荟新苷 D |
Beta-Secretase; BACE | Neuroscience |
Aloeresin D 是一种从芦荟中分离得到的色原酮苷,能够抑制 β-分泌酶活性,IC50=39 μM。 | |||
TN2190 |
Scoulerine
|
Apoptosis; Beta-Secretase; BACE; Parasite | Apoptosis; Microbiology/Virology; Neuroscience |
Scoulerine 是抗有丝分裂化合物。它抑制细胞增殖,阻止细胞周期,并诱导癌细胞凋亡。它也是BACE1(淀粉样前体蛋白裂解酶 1) 的抑制剂。 | |||
T2S1181 |
Aloenin
Aloenin A,Aloearbonaside,芦荟宁 |
Beta-Secretase; AChR | Neuroscience |
Aloenin (Aloenin A) A 是一种具有清除过氧自由基作用的天然产物,对 β-分泌酶 (BACE) 具有中等抑制活性。 | |||
TN2217 |
Sophoflavescenol
槐苦参醇,槐黄醇 |
Others; Beta-Secretase; BACE; PDE; AChR; AChE | Metabolism; Neuroscience; Others |
Sophoflavescenol 是异戊烯基黄酮类化合物,能够抑制PDE5的活性,IC50=0.013 μM。它也抑制 RLAR,HRAR,BACE1,AChE 和 BChE,IC50值分别为 0.30 µM,0.17 µM,10.98 µM,8.37 µM 和 8.21 µM。 | |||
T8306 |
Epiberberine chloride
表小檗碱氯化物,Epiberberine (chloride),盐酸表小檗碱 |
Reactive Oxygen Species; Beta-Secretase; BACE; AChR; AChE | Immunology/Inflammation; Metabolism; Neuroscience; NF-κB |
Epiberberine chloride (Epiberberine (chloride)) 是一种从黄连中得到的生物碱,是一种AChE 和BChE 抑制剂,和非竞争性的BACE1抑制剂。它具有抗氧化作用,能够清除 ONOO-,可用于研究阿尔滋海默症和糖尿病。 | |||
T4753 |
Imidazoleacetic acid hydrochloride
I4AA,(4-Imidazolyl)acetic acid hydrochloride,4-咪唑乙酸盐酸盐,4-Imidazoleacetic acid hydrochloride |
Endogenous Metabolite; Antibiotic | Metabolism; Microbiology/Virology |
Imidazoleacetic acid hydrochloride (I4AA) 是咪唑衍生物,具有潜在的抗结核性能。它还用于制备β-分泌酶的酰基胍抑制剂。 | |||
T4115 |
Auraptene
橙皮油内酯,7-geranyloxycoumarin,橙皮油素 |
MMP; BACE | Neuroscience; Proteases/Proteasome |
Auraptene 是一种丰富的天然香叶氧基香豆素。它能够抑制基质金属蛋白酶 2 以及关键炎症因子,包括 IL-6,IL-8 和趋化因子 (C-C 基序) 配体-5 (CCL5)的分泌。 |