Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
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)。 | |||
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. | |||
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。 | |||
T11360 |
gamma-secretase modulator 3
|
Others | Others |
gamma-secretase modulator 3 is a gamma-secretase modulator. | |||
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. | |||
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。 | |||
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。 | |||
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。 | |||
T11358L |
gamma-secretase modulator 1 hydrochloride
gamma-secretase modulator 1 hydrochloride (1172637-87-4 free base) |
Others | Others |
gamma-secretase inhibitior-1 是γ-secretase 调节剂,gamma-secretase inhibitior-1可用于阿尔茨海默病。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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. | |||
T40315 | γ-Secretase modulator 10 | ||
γ-Secretase modulator 10 is a novel 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. | |||
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. | |||
T39702 |
RO7185876
RO7185876 |
||
RO7185876 is a potent and selective gamma secretase modulator as a potential treatment for Alzheimer's disease. | |||
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。 | |||
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。 | |||
T31999 | GSI-136 | ||
GSI-136 is a gamma secretase inhibitor. | |||
T26706 |
AZ4800
AZ-4800,AZ 4800 |
||
AZD4800 is a gamma secretase modulators. | |||
T70635 | ELND007 | ||
ELND007 is a Gamma secretase inhibitor. | |||
T14525 |
Begacestat
GSI-953 |
Beta Amyloid | Neuroscience |
Begacestat is a selective thiophene sulfonamide amyloid precursor protein gamma-secretase inhibitor (Aβ40,IC50=15 nM),and for the treatment of Alzheimer's disease. | |||
T31733 |
EVP-0015962
|
||
EVP-0015962, which is bioavailable orally, is a potent and selective gamma-secretase regulator in vitro and in vivo, detectable in the brain. | |||
T39492 |
FRM-024
|
||
FRM-024 is a potent CNS-penetrant gamma secretase modulator for familial Alzheimer’s disease. | |||
T29233 |
Z-LLNle-CHO
|
||
Z-LLNle-CHO is a cell permeable inhibitor of gamma-secretase. Z-LLNle-CHO induces apoptosis of human glioblastoma tumor-initiating cells by proteasome inhibition and mitotic arrest response. | |||
T2625L |
MK-0752 Sodium
MK 0752,MK0752,MK-0752 |
||
Sodium MK-0752 is a novel and potent gamma-secretase inhibitor that has been evaluated in clinical trials for the treatment of various types of cancer. | |||
T38266 |
Nirogacestat dihydrobromide
|
||
Potent γ-secretase inhibitor (IC50 values are 1.2 and 6.2 nM in whole cell and cell-free assays, respectively). Reduces Aβ in brain, CSF and plasma in mice and guinea pigs. Lanz et al (2010) Pharmacodynamics and pharmacokinetics of the gamma-secretase inhibitor PF-3084014. J.Pharmacol.Exp.Ther. 334 269 PMID:20363853 | |||
T70951 |
ELND006
|
||
ELND006 is a novel gamma secretase inhibitor previously under investigation for the oral treatment of Alzheimer's disease. ELND006 shows poor solubility and has moderate to high permeability. The in vivo performance of the ELND006 nanosuspension was tested in fed and fasted beagle dogs and compared with a gelatin capsule containing reference API. The results show that nanosizing ELND006 profoundly improved the oral bioavailability and virtually eliminated variation resulting from food intake. | |||
T76393 |
Amyloid 17-42
|
||
Amyloid 17-42 (Aβ(17-42)),作为阿尔茨海默病中弥漫性斑块与唐氏综合症小脑前区的主要淀粉样蛋白成分,源于淀粉样蛋白前体蛋白(APP)经α与γ分泌酶的裂解作用。此外,Amyloid 17-42能通过Fas样/caspase-8途径促使神经细胞发生凋亡。 |