Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T40315 | γ-Secretase modulator 10 | ||
γ-Secretase modulator 10 is a novel γ-secretase modulator. | |||
T11361 | γ-Secretase modulator 4 | Others | Others |
γ-Secretase modulator 4 is a potent γ-secretase modulator, reduces the Aβ42 level with IC50s of 0.017 μM and 0.014 μM in mouse and human, respectively. | |||
T9422 |
Fosciclopirox
CPX-POM |
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
Fosciclopirox (CPX-POM) 利用靶向γ-分泌酶,抑制尿路上皮癌的生长。静脉给药后,它选择性地将活性代谢物 Ciclopirox 递送至整个尿路。Ciclopirox 在许多实体和血液恶性肿瘤中显示出抗癌活性。 | |||
T16294 |
NGP555
|
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
NGP555 是 γ-分泌酶调节剂。 | |||
T6063 |
LY-411575
LY411575 |
Apoptosis; Gamma-secretase | Apoptosis; Neuroscience; Proteases/Proteasome; Stem Cells |
LY-411575 是一种高效的γ-secretase 抑制剂,能够抑制 Aβ40 蛋白的产生,在膜中的 IC50 为 0.078 nM,在细胞中为 0.082 nM。 它还抑制 Notch 切割,IC50 为 0.39 nM。 | |||
T6249 |
Avagacestat
BMS-708163 |
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
Avagacestat (BMS-708163) 是一种有效的γ-secretase 抑制剂,抑制 Aβ42 (IC50:0.27 nM) 和 Aβ40 (IC50:0.30 nM) 的产生。它同时抑制 Notch 胞内结构域 (NICD) (IC50:0.84 nM) 和 CYP2C19 (IC50:20 nM) 。它可用于阿尔兹海默症的研究。 | |||
T6135 |
YO-01027
gamma-Secretase Inhibitor XX,Dibenzazepine,DBZ,二苯并氮卓 |
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
YO-01027 (DBZ) 是一种高效的 γ-分泌酶抑制剂,能够裂解 Notch (IC50:2.92 nM) 和 APPL (IC50:2.64 nM)。 | |||
T2625 |
MK-0752
|
Beta Amyloid; Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
MK0752 是一种高效的、特异性的、可穿过血脑屏障的、口服活性的 γ-分泌酶(γ-secretase)抑制剂,对人 SH-SY5Y 细胞 Aβ40 呈剂量依赖性降低(IC50=5 nM)。它能够降低体内新生的中枢神经系统 Aβ。 | |||
T3633 |
Crenigacestat
LY3039478 |
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
Crenigacestat (LY3039478) 是一种口服具有活性的Notch 和γ-secretase 的抑制剂,其在多种肿瘤细胞中的IC50为 ∼1nM。 | |||
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。 | |||
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。 | |||
T16133 |
MRK-560
|
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
MRK-560 是高效的、口服有效的 γ- 分泌酶抑制剂抑制剂,具有大脑屏障渗透性。 | |||
T6274 |
RO4929097
RG-4733 |
Beta Amyloid; Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
RO4929097 (RG-4733) 是 γ secretase 抑制剂,IC50=4 nM,能够抑制细胞内 Aβ40 (EC50:14 nM) 的产生和 Notch (EC50:5 nM) 活性。 | |||
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。 | |||
T2262 |
Itanapraced
CHF5074,CSP-1103 |
Beta Amyloid; Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
Itanapraced (CHF5074) 是新型γ-secretase 调节剂,能够降低 Aβ42 (IC50=3.6 nM) 和 Aβ40 (IC50=18.4 nM) 分泌。 | |||
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。 | |||
T6935 |
Nirogacestat
PF-03084014,PF-3084014,PF03084014,PF 03084014 |
Apoptosis; Gamma-secretase | Apoptosis; Neuroscience; Proteases/Proteasome; Stem Cells |
Nirogacestat (PF 03084014) 是一种具有口服活性的,可逆的,非竞争性的,选择性γ-secretase 抑制剂,IC50为 6.2 nM。它抑制 Notch 信号通路,可研究 Notch 受体依赖性肿瘤。 | |||
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。 | |||
T22678 |
3,5-Bis(4-nitrophenoxy)benzoic acid
3,5-二(4-硝基苯氧基)苯甲酸,Compound W |
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
3,5-Bis(4-nitrophenoxy)benzoic acid (Compound W) 是 γ-secretase 抑制剂。它导致 Aβ42 和 notch-1 Aβ-like peptide 25 (Nβ25) 的释放水平降低。它是母体血清中 3,3’-diiodothyronine sulfate (T2S) 的交叉反应物质,可作为胎儿甲状腺功能减退的标志物。 | |||
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. | |||
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]. | |||
T17281 |
Z-Ile-Leu-aldehyde
Z-IL-CHO,GSI-XII,γ-Secretase inhibitor XII |
Others | Others |
Z-Ile-Leu-aldehyde is an effective and competitive peptide aldehyde inhibitor of γ-secretase and notch. | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
T14690 |
BMS 433796
BMS-289948,BMS-299897 |
Beta Amyloid | Neuroscience |
BMS 433796 是一种在阿尔茨海默病转基因小鼠模型中具有Aβ降低活性的γ分泌酶抑制剂,可有效抑制 Aβ 的产生。 | |||
T10532 |
BI-1408
|
Others; Gamma-secretase | Neuroscience; Others; Proteases/Proteasome; Stem Cells |
BI-1408 是一种强效的 γ 分泌酶调节剂(对 Aβ42 的 IC50 值为 0.04 μM)。 | |||
T9015 |
LY900009
|
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
LY900009 是一种通过选择性抑制 γ-分泌酶蛋白来抑制 Notch 信号传导的小分子抑制剂。 | |||
T9641 |
Aβ42-IN-2
|
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
Aβ42-IN-2 是一种 γ-secretase 调节剂。Aβ42-IN-2 对 Αβ42 的 IC50 值为 6.5 nM 。Aβ42-IN-2 可用于阿尔茨海默症相关的研究。 | |||
T11178L |
ELN318463 racemate
ELN318463 (racemate),ELN 318463 racemate |
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
ELN318463 racemate (ELN 318463 racemate) 是 ELN318463 的外消旋体,ELN318463 是一种淀粉样前体蛋白 (APP) 选择性 γ-分泌酶抑制剂。 | |||
T14673 |
BMS 299897
|
Beta Amyloid; Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
BMS 299897 是一种磺胺类 γ 分泌酶抑制剂。它在稳定过表达淀粉样前体蛋白(APP)的 HEK293 细胞中抑制 Aβ 生成的 IC50 值为 7 nM。 | |||
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。 | |||
T63208 |
Aβ-IN-1
|
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
Aβ-IN-1 是一种新型有效且具有口服活性的 γ 分泌酶调节剂 (GSM)。 Aβ-IN-1 在不抑制 CYP3A4 的情况下,在培养细胞中有效降低 Aβ42 水平,IC50值为 0.091 μM。Aβ-IN-1 显示出良好的药代动力学特征。 | |||
T14680 |
BMS-906024
Osugacestat,AL-101,BM-0018 |
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
BMS-906024 (Osugacestat) 是一种可口服且具有选择性的γ 分泌酶抑制剂,是一种小分子 Notch 抑制剂。BMS-906024 对多种人类癌症异种移植具有广谱抗肿瘤活性。BMS-906024 可阻止所有四种 Notch 受体的激活,对 Notch1、-2、-3 和 -4 受体的 IC50 分别为 1.6、0.7、3.4 和 2.9 nM。 | |||
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。 | |||
T2470 |
MDL-28170
Calpain Inhibitor III |
Cysteine Protease; Proteasome | Proteases/Proteasome; Ubiquitination |
MDL-28170 (Calpain Inhibitor III) 是一种选择性的、有效的、具有膜渗透性的半胱氨酸蛋白酶 (calpain)抑制剂,可在全身给药后迅速穿过血脑屏障。它还能阻断γ-secretase。 | |||
T13037 |
Sulindac sulfide
cis-Sulindac sulfide |
Raf; Others; AChR | MAPK; Neuroscience; Others |
Sulindac sulfide (cis-Sulindac sulfide) 是一种非甾体抗炎化合物,对COX-1具有很高的亲和力,是Ras 激活Raf-1的抑制剂。Sulindac sulfide 是 γ-secretase 的一个非竞争性抑制剂, IC50 为 20.2 μM。它是舒林酸的活性代谢物。 | |||
T11178 |
ELN318463
ELN 318463 |
Others | Others |
ELN 318463 shows differential inhibition of presenilin (PS1)- and PS2-comprised γ-secretase with EC50s of 12 nM and 656 nM for PS1 and PS2, respectively. ELN 318463 is 51-fold more selective for PS1.ELN 318463 is an amyloid precursor protein (APP) selective γ-secretase inhibitor. | |||
T23431 |
TC-E 5006
|
Others | Others |
γ-secretase modulator | |||
T11359 | gamma-secretase modulator 2 | Others | Others |
gamma-secretase modulator 2 is a potent and selective γ-secretase modulator for treatment of Alzheimer's disease .γ-secretase modulator is modulation of the action of γ-secretase so as to Selectively attenuate production of Aβ(1-42) and hence find use in treatment or prevention of diseases associated with deposition of Aβ in the brain. γ-secretase modulator is usful in particular Alzheimer's disease. | |||
T26864 |
BMS-932481
BMS932481 |
||
BMS-932481 is a γ-secretase modulator. | |||
T24116 |
GSM-1
gamma Secretase modulator 1,GSM 1 (enzyme modulator),J2.559.799K |
||
GSM-1 is a modulator of γ-Secretase. |