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Cat. No. | Product Name | Target | Signaling Pathways |
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T17011 |
TCH-165
|
Proteasome | Proteases/Proteasome; Ubiquitination |
TCH-165 是一种蛋白酶体组装的小分子调节剂,可增加游离 20S 水平,进而增强 IDP 蛋白水解。 | |||
T71611 | αSyn-IN-576755 | ||
αSyn-IN-576755 is a novel inhibitor of αSyn fibrillization, blocking fibril growth and suppressing A53T αSyn neurotoxicity. | |||
T61787 |
SYN20028567
|
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SYN20028567, an aromatase (CYP19) inhibitor, exhibits an IC50 value of 9.4 nM. It has potential applications in breast cancer research [1]. | |||
T83726 |
Tat-βsyn-degron TFA
|
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Tat-βsyn-degron是一种降低α-synuclein表达的肽。其结构包括HIV-1 Tat质膜跨导域、与β-synuclein氨基酸36-45相对应的α-synuclein结合域βsyn,以及蛋白酶体定向域degron。在肽-蛋白结合实验中,Tat-βsyn-degron能够与重组α-synuclein结合,并在大鼠初级皮质神经元培养中降低α-synuclein水平,这一效应可以通过蛋白酶体抑制剂MG132阻止。体内研究显示,Tat-βsyn-degron (40 mg/kg)能够在过表达人类A53T突变体α-synuclein的M38转基因小鼠的大脑中降低α-synuclein水平,并且在黑质和脑桥中降低磷酸化α-synuclein水平,以及在通过α-synuclein预成纤维诱导的扩散性α-synuclein病理模型小鼠中减少神经炎症。此外,Tat-βsyn-degron (6 µmol/kg, i.p.)在MPTP诱导的帕金森病小鼠模型中,保护多巴胺能神经元,缓解运动缺陷。 | |||
T23709 |
alphaSYN-IN-NAB2
alphaSYN inhibitor NAB2,alphaSYNINNAB2,alphaSYN-IN-NAB2,NAB2,alphaSYN inhibitor-NAB2 |
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alphaSYN-IN-NAB2 是一种神经元保护剂,是一种由 NAB2基因编码的蛋白质。NAB2 高效且具有选择性地保护多种细胞免受 α-syn 毒性。NAB2 对依赖于 E3 泛素连接酶 Rsp5/Nedd4 的内体转运具有促进作用。NAB2 确定 α-syn 生物学中的一个可活性分子节点,该节点可以纠正其潜在病理学的多个方面,包括功能失调的内体和内质网到高尔基体囊泡的运输。NAB2参与细胞分化、凋亡和应激反应等细胞过程,可用来研究癌症、神经发育和神经元活动。 | |||
T6708 |
Tolcapone
Tasmar,Ro 40-7592,托卡朋 |
Apoptosis; Beta Amyloid; Transferase | Apoptosis; Metabolism; Neuroscience |
Tolcapone (Ro 40-7592) 是一种选择性,具有口服活性的外周和中枢COMT 抑制剂,在肝脏中对 COMT 的IC50为 773 nM。它还是一种 α-syn 和 Aβ42 寡聚和原纤维形成的有效抑制剂,可诱导氧化应激导致神经母细胞瘤细胞凋亡和抑制肿瘤生长。 | |||
T61404 |
α-Synuclein inhibitor 3
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α-Synuclein inhibitor 3 (Compound 7g) is a potent inhibitor of α-synuclein (α -Syn) aggregation. It has potential applications in Parkinson's disease research [1]. | |||
T63244 |
MG-2119
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MG-2119 是单体 tau 和 α-syn aggregation 的有效抑制剂,能够用于研究神经疾病。 | |||
T62131 |
α-Synuclein inhibitor 5
|
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α-Synuclein inhibitor 5 是一种有效的、能够透过血脑屏障的 α-Synuclein (α-Syn) 聚集的抑制剂 (IC50: 1.22 μM),在 30 μM 时的抑制率为 94.3%。 | |||
T61920 | α-Synuclein inhibitor 7 | ||
α-Synuclein inhibitor 7 (化合物 3gf) 是有效的α-Synuclein (α-Syn)聚集的抑制剂,IC50为 1.95 μM,30 μM 处的抑制率为 85.8%。α-Synuclein inhibitor 7具有血脑屏障通透性。 | |||
T74974 | SQ-3 | ||
SQ-3为一种喹啉类似物,对α-syn聚合体(Ki=39.3 nM)显示中等选择性,其选择性高于对β-淀粉样蛋白(Aβ)聚合体(Ki=230 nM)。[18F]SQ3展现出作为α-syn成像探针的先导化合物的基本属性。 | |||
T62414 | Dyrk1A-IN-1 | ||
Dyrk1A-IN-1 是一种具有 Dyrk1A 激酶活性、tau 和 α-syn 寡聚物的聚集的三重性抑制剂,对 Dyrk1A 激酶的 IC50 值为 119 nM。 | |||
T81031 | tau protein/α-synuclein-IN-1 | ||
tau protein/α-synuclein-IN-1为tau protein与α-synuclein双重抑制剂,能够抑制M17D神经母细胞瘤细胞中α-syn包涵体的形成,适用于阿尔茨海默病相关研究。 | |||
T61644 | α-Synuclein inhibitor 6 | ||
α-Synuclein inhibitor 6 (compound 3ge) is a highly effective and blood-brain barrier-permeable inhibitor that targets the aggregation of α-Synuclein (α-Syn). It exhibits a potent inhibitory activity, with an IC50 value of 1.70 μM, leading to a remarkable inhibition ratio of 94.4% at 30 μM [1]. | |||
T74770 | D-685 | ||
D-685作为D-520的前体药物,在帕金森病(PD)血脂化动物模型中展示了优于D-520的体内抗PD功效。此外,D-685能降低人类α-突触核蛋白(α-syn)的累积,且具有更高的大脑透过性。 | |||
T71174 |
PBT434 HBr
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PBT434 is a novel, brain-penetrant, small molecule inhibitor of α-synuclein aggregation. In transgenic animal models of Parkinson disease (A53T) and MSA (PLP-α-Syn), PBT434 reduced α-synuclein aggregation, preserved neurons and improved motor function. Glial cell inclusions were also reduced in a murine MSA model. PBT434 is thought to act by redistributing reactive iron across membranes, thereby blocking intracellular protein aggregation and oxidative stress. The affinity of PBT434 for iron is g... | |||
T11207 | Entacapone sodium salt | Others | Others |
Entacapone sodium salt inhibits catechol-O-methyltransferase(COMT) with similar IC50 in different tissues including live, duodenum, kidney and lung, but entacapone is more active than tolcapone in those tissues. Entacapone (< 100 μM) is a potent inhibitor of α-syn and β-amyloid (Aβ) oligomerization and fibrillogenesis, and also protects against extracellular toxicity induced by the aggregation of both proteins in PC12 cells.Entacapone sodium salt is a specific, potent, peripherally acting catech... | |||
T78842 | α-Synuclein inhibitor 9 | ||
α-Synuclein inhibitor9 (Compound 20C) 是一种针对 α-Synuclein 的抑制剂,通过与成熟 α-Synuclein 原纤维内的空腔结合,减少了 β-折叠构型,并有效阻止 A53T α-Syn 的聚集。由于其神经保护性质,该化合物能够改善大脑功能性连接并缓解运动障碍,适用于帕金森病 (PD) 的相关研究。 |
Cat. No. | Product Name | Target | Signaling Pathways |
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T72962 |
Sycosterol A
|
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Sycosterol A 是一种α-synuclein(α-syn)甾醇抑制剂。 | |||
T82478 |
Ellagic acid 4-O-α-L-arabinopyranoside
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Ellagic acid 4-O-α-L-arabinopyranoside,一种具有抗氧化活性的化合物,从Dimocarpus longan Lour, syn. Euphoria longan Lam.(龙眼)中分离得到。 |