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36

抑制剂 & 化合物

2

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Cat. No.	Product Name	Target	Signaling Pathways
T5447	Anle138b	Beta Amyloid; Others	Neuroscience; Others
	Anle138b 是一种毒性低，口服生物利用度高，血脑屏障通透性好的低聚物聚集抑调节剂，可阻断朊病毒蛋白和 α-突触核蛋白病理性聚集的形成。它在体内强烈抑制低聚物积累、神经元变性和疾病进展。它阻断 Aβ 通道并挽救淀粉样变性小鼠模型的疾病表型。
T2238	Cariporide 卡立泊来德,HOE-642	Sodium Channel	Membrane transporter/Ion channel
	Cariporide (HOE-642) 是一种选择性的Na+/H+交换抑制剂。
T77478	Milatuzumab hLL1,MEDI-115	Others	Others
	Milatuzumab (MEDI-115) 是一种人源化抗 CD74 单克隆抗体。Milatuzumab 促使自由基氧的产生和线粒体膜电位的丧失，可降低 CD20/CD74 聚集体和细胞粘附，诱导细胞死亡。
T22694	CRANAD 2	Others	Others
	CRANAD 2 是一种特异性近红外 (NIR) 荧光探针，可用于检测 Aβ 斑块。它可透过血脑屏障，且对 Aβ 聚集体有高亲和性，其 Kd=38 nM。
T38861L	Tat-beclin 1 acetate Tat-beclin 1 acetate(1423821-88-8 free base)	HIV Protease; Autophagy	Autophagy; Microbiology/Virology; Proteases/Proteasome
	Tat-beclin 1 acetate 是一种有效的自噬诱导剂，并与自噬的负调节因子 GAPR-1 相互作用。 Tat-beclin 1 acetate 减少聚谷氨酰胺扩增蛋白聚集体的积累和几种病原体（包括 HIV-1）的复制。
T10782	CGP52411 DAPH	EGFR; Beta Amyloid	Angiogenesis; JAK/STAT signaling; Neuroscience; Tyrosine Kinase/Adaptors
	CGP52411 是一种具有口服活性的 ATP 竞争性 EGFR 抑制剂（IC50：0.3 μM）。 CGP52411 阻止 Ca2+ 离子有毒流入神经元细胞，并显着抑制和逆转 β-淀粉样蛋白 Aβ42 原纤维聚集体的形成。 CGP52411 可用于阿尔茨海默病的研究。
T62899	Tau-aggregation and neuroinflammation-IN-1	Microtubule Associated; NO Synthase	Cytoskeletal Signaling; Immunology/Inflammation
	Tau-aggregation and neuroinflammation-IN-1 是一种有效的 Tau 蛋白聚集体抑制剂，对 AcPHF6 和全长 tau 蛋白聚集体显示出显著的抑制活性。Tau-aggregation and neuroinflammation-IN-1具有抗炎活性且可减少 NO 释放。Tau-aggregation and neuroinflammation-IN-1 对 LSP 刺激的 BV2 细胞具有低细胞毒性。Tau-aggregation and neuroinflammation-IN-1 可逆转冈田酸诱导的大鼠记忆障碍。
T11191	EN6	Proton pump; Autophagy	Autophagy; Membrane transporter/Ion channel
	EN6 是一种小分子体内自噬激活剂，其共价靶向溶酶体v-ATP 酶的 ATP6V1A 亚基中的半胱氨酸 277。它以溶酶体依赖性方式清除 TDP-43 聚集体，这是额颞叶痴呆的病原体。它介导的 ATP6V1A 修饰使 v-ATP 酶与 Rags 分离，从而抑制 mTORC1 信号传导、增加溶酶体酸化和激活自噬。
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。
T34766	T-808 AVI-680
	T-808 is a tau tracer which may be used in radiographic labeling of Tau aggregates during Alzheimer's disease.
T35151	X-34 X 34
	X-34 is a highly fluorescent amyloid-specific dye, exhibiting inclusion bodies that were amyloid-like aggregates by virtue of their staining.
T37051	Tau tracer 2
	Tau tracer 2 (Pl-2620) is a specific imaging agent designed to detect and visualize Tau protein aggregates. Its primary application lies in the diagnosis of neurodegenerative diseases [1].
T20821	EPPS
	EPPS is a rescuer of A aggregation and behavioral deficits. It binds to A aggregates and converts them into monomers.
T69149	L2-b
	L2-b is a bifunctional Aβ-interacting, metal-chelating molecule that modulates ROS production in, and improves survival of neuroblastoma cells incubated in the presence of Aβ along with Copper or Zinc. In cell-free aggregation studies, L2-b inhibits metal-induced Aβ aggregation, and also promotes the dissociation of Ab aggregates in homogenates of human AD brain samples.
T39660	Tau tracer 1
	Tau tracer 1 is a radiopharmaceutical agent designed specifically for visualizing Tau protein aggregates, commonly associated with neurodegenerative diseases. Its primary application lies in the diagnosis of these conditions.
T80700	β Amyloid(17-28) human
	β Amyloid(17-28) human 为β-淀粉样肽(Abeta)的一段核心片段，其结构受脂质诱导。本化合物能够促进β Amyloid40全长肽段的聚集，导致阿尔茨海默病(AD)中具毒性的聚集体形成。
T61206	AChE/BChE/BACE-1-IN-1
	AChE/BChE/BACE-1-IN-1 (Compound 4k) is an orally active inhibitor that targets acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-site amyloid precursor protein cleaving enzyme 1 (BACE-1). It displays IC50 values of 0.058 μM, 0.082 μM, and 0.115 μM against hAChE, hBChE, and hBACE-1, respectively. AChE/BChE/BACE-1-IN-1 exhibits significant binding affinity with PAS-AChE, excellent ability to cross the blood-brain barrier, potential disassembly of amyloid-beta (Aβ) aggregates, and ne...
TP1225	β-Amyloid (22-35) β-Amyloid 22-35,Amyloid β-Protein (22-35)
	β-Amyloid (22-35) is a 14-aa peptide, shows aggregates and induces neurotoxicity in the hippocampal cells. Beta amyloid (22-35) is a synthetic truncated fragment of beta-amyloid peptide.
T61087	THK-5105
	THK-5105为芳基喹啉衍生物，具备与tau原纤维高度结合的亲和力。它对tau蛋白聚集体及含tau的阿尔茨海默病(AD)脑匀浆显示出显著的结合能力。18F-THK-5105展现出作为tau成像PET探针的潜能。
T60907	THK-5117
	THK-5117 是一种芳基喹啉衍生物，具有作为 tau 成像 PET 探针的潜力。THK-5117 对 tau 原纤维表现出高结合亲和力，Ki 值为 10.5 nM。THK-5117 还显示出对 tau 蛋白聚集体和富含 tau 的阿尔茨海默病 (AD) 脑匀浆的高结合亲和力。
T38764	Amylin (8-37), human
	Amylin (8-37), human, derived from human Amylin, possesses direct vasodilator effects in isolated mesenteric resistance arteries of rats. Human Amylin is a small pancreatic β-cell hormone that forms aggregates in the absence of insulin and is a key pathological feature of type II diabetes mellitus.
T75958	β-Amyloid (22-35) (TFA)
	β-Amyloid 22-35 (Amyloid β-Protein 22-35) TFA是β-淀粉样蛋白22-35残基段，具细胞毒性，能影响无血清培养大鼠海马神经元。在中性缓冲液中，此化合物能形成聚集体与典型淀粉样纤维，模拟β-淀粉样蛋白行为。
T76725	Tilavonemab
	Tilavonemab (ABBV-8E12) 是一种人源化抗 tau 抗体，结合 tau 蛋白 N 端附近的 25-30 位氨基酸。Tilavonemab 阻断人和小鼠神经元摄取 tau 聚集体的能力，并能减少脑萎缩。Tilavonemab 可用于阿尔兹海默症的研究。
T35507	12-HETE
	(±)12-HETE is one of the six monohydroxy fatty acids produced by the non-enzymatic oxidation of arachidonic acid. The biological activity of (±)12-HETE is similar to that of its constituent enantiomers . It aggregates neutrophils with an EC50 value of 40 nM.[1] Reference：[1]. O'Flaherty, J.T., Thomas, M.J., Lees, C.J., et al. Neutrophil-aggregating activity of monohydroxyeicosatetraenoic acids. American Journal of Pathology 104, 55-62 (1981).
T73533	ADH-6
	ADH-6，一种三吡啶酰胺化合物，消除突变p53 DBD聚集成核亚结构域的自组装，并靶向解离人类癌细胞中的突变p53聚集体。通过此过程，ADH-6恢复p53的转录活性，导致细胞周期停滞与细胞凋亡(apoptosis)，展示了其研究癌症疾病的潜力。
T73912	Maysin
	Maysin 是一种具有神经保护作用的 C-糖基黄酮，可以从玉米须中分离得到。Maysin 对 Syn 淀粉样蛋白聚集体-低聚物和原纤维引起的损伤具有保护作用。Maysin 可防止氧化应激和细胞内钙稳态失衡，激活自噬降解过程。Maysin 可用于帕金森病(PD) 的研究。
T79250	PROTAC α-synuclein degrader 5	PROTACs	PROTAC
	PROTACα-synuclein degrader 5为针对α-synuclein聚集体的高度选择性小分子(PROTAC)，具有DC50值为7.51 μM和最大降解率Dmax达89%。该化合物结合了探针分子sery308与E3 ligase链接剂，适用于神经系统疾病研究。
T74443	ADH-6 TFA
	ADH-6 TFA为三吡啶酰胺类化合物，通过靶向并解离人类癌细胞中突变p53聚集体，阻止突变p53 DBD聚集成核亚结构域的自组装，从而恢复p53的转录活性。这一过程导致细胞周期停滞和细胞凋亡(apoptosis)，显示出其在研究癌症疾病中的应用潜力。
T61063	SEN177
	SEN177 在亨廷顿病的研究中显示出潜力。它是谷氨酰胺环化酶 (QPCT) 的有效抑制剂，对谷氨酰胺肽环转移酶 (QPCTL) 的 IC50值为 0.013 μM。SEN177 对人谷氨酰胺环化酶 (hQC) 的 Ki 值为 20 nM。SEN177 显著降低了突变 HTT 寡聚化的早期阶段，并降低了具有 Q80 聚集体的神经元的百分比。
T38861	Tat-beclin 1
	Tat-beclin 1, a peptide derived from the autophagy protein beclin 1, is a powerful inducer of autophagy. It interacts with GAPR-1 (GLIPR2), a negative regulator of autophagy. Tat-beclin 1 effectively reduces the buildup of polyglutamine expansion protein aggregates and inhibits the replication of various pathogens, such as HIV-1, in laboratory experiments. In addition, it has demonstrated the ability to decrease mortality in mice infected with chikungunya (CHIKV) or West Nile virus (WNV).
T75378	DCDAPH
	DCDAPH（Compound 2c）是用于β-淀粉样蛋白（Aβ）斑块检测的新型智能近红外探针，在PBS中λex/λem为597/665 nm。此化合物对Aβ具有高亲和性（Ki=37 nM，Kd=27 nM），并显示良好的血脑屏障渗透性，能够满足大多数体外及体内Aβ检测需求。
TP1152	Fibronectin Adhesion-promoting Peptide TFA Heparin Binding Peptide TFA
	Fibronectin Adhesion-promoting Peptide (Heparin Binding Peptide) is one of the heparin-binding amino acid sequences found in the carboxy-terminal heparin-binding domain of fibronectin. It promotes assembly of mesenchymal stem cell (MSC) spheroids into lar
T60691	AChE/BChE/BACE-1-IN-2
	AChE/BChE/BACE-1-IN-2 (Compound 4o) 表现出显著的抗氧化潜力和对PAS-AChE 的强大的结合能力。AChE/BChE/BACE-1-IN-2 是口服有效的AChE、BACE-1和BChE 抑制剂，对 hAChE、hBACE-1 和hBChE 的IC50分别为 0.069、0.097 和0.127 μM。AChE/BChE/BACE-1-IN-2 显示出对潜在的 Aβ 聚集物的分解能力和针对 Aβ 诱导的应激的神经保护作用。
T81803	MFN2 agonist-1
	MFN2 agonist-1 (B-A/l) 是一种有效促进缺陷细胞中MFN2表达的化合物，能够促进线粒体融合。在表达CMT2A突变型MFN2 T105M的小鼠培养神经元中，MFN2 agonist-1能够逆转线粒体的“聚集”现象（指静态线粒体聚集体的形成）并恢复其运动性。
T76058	Tat-beclin 1 TFA
	Tat-beclin 1 TFA是一种来源于自噬蛋白区域(beclin 1)的肽，有效诱导自噬(autophagy)并与GAPR-1 (GLIPR2)发生相互作用，具有显著的自噬负调控作用。该化合物能有效减少体外聚谷氨酰胺扩增蛋白聚集体的积累，并抑制HIV-1等多种病原体的复制。同时，Tat-beclin 1 TFA能显著降低感染基孔肯雅病(CHIKV)或西尼罗河病毒(WNV)小鼠的死亡率。
T35627	Amylin (human) (trifluoroacetate salt)
	Amylin is a 37-residue peptide hormone secreted from pancreatic β-cells that reduces food intake, decreases glucagon secretion, slows gastric emptying, and increases satiety. It binds to amylin receptors with IC50 values of 2 and 0.2 nM for porcine and guinea pig nucleus accumbens membrane preparations, respectively. Amylin is present in amyloid aggregates derived from the pancreatic islets of humans with type 2 diabetes. Amylin forms fibrils that react to thioflavin T and are organized in a cro...

化合物

Cat.No: T5447

Target: Beta Amyloid, Others

Cat.No: T2238

Synonym: 卡立泊来德,HOE-642

Target: Sodium Channel

Cat.No: T77478

Synonym: hLL1,MEDI-115

Target: Others

Cat.No: T22694

Target: Others

Tat-beclin 1 acetate

Cat.No: T38861L

Synonym: Tat-beclin 1 acetate(1423821-88-8 free base)

Target: HIV Protease, Autophagy

Cat.No: T10782

Synonym: DAPH

Target: EGFR, Beta Amyloid

Tau-aggregation and neuroinflammation-IN-1

Cat.No: T62899

Target: Microtubule Associated, NO Synthase

Cat.No: T11191

Target: Proton pump, Autophagy

Cat.No: T74974

Cat.No: T34766

Synonym: AVI-680

Cat.No: T35151

Synonym: X 34

Cat.No: T37051

Cat.No: T20821

Cat.No: T69149

Cat.No: T39660

β Amyloid(17-28) human

Cat.No: T80700

AChE/BChE/BACE-1-IN-1

Cat.No: T61206

β-Amyloid (22-35)

Cat.No: TP1225

Synonym: β-Amyloid 22-35,Amyloid β-Protein (22-35)

Cat.No: T61087

Cat.No: T60907

Amylin (8-37), human

Cat.No: T38764

β-Amyloid (22-35) (TFA)

Cat.No: T75958

Cat.No: T76725

Cat.No: T35507

Cat.No: T73533

Cat.No: T73912

PROTAC α-synuclein degrader 5

Cat.No: T79250

Target: PROTACs

Cat.No: T74443

Cat.No: T61063

Cat.No: T38861

Cat.No: T75378

Fibronectin Adhesion-promoting Peptide TFA

Cat.No: TP1152

Synonym: Heparin Binding Peptide TFA

AChE/BChE/BACE-1-IN-2

Cat.No: T60691

Cat.No: T81803

Tat-beclin 1 TFA

Cat.No: T76058

Amylin (human) (trifluoroacetate salt)

Cat.No: T35627

Cat. No.	Product Name	Target	Signaling Pathways
T37957	Setosusin
	Setosusin is a meroterpenoid fungal metabolite originally isolated from C. setosus. It reduces neurotoxicity induced by amyloid-β (Aβ) aggregates in PC12 cells (EC50 = 112.6 μM). In vivo, setosusin (30 mg/kg) induces tremors in mice.
TN1533	Cucurbitacin A	ROCK	Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells
	Cucurbitacin I, cytotoxic triterpenoid sterols isolated from plants, elicits the formation of actin/phospho-myosin II co-aggregates by stimulation of the RhoA/ROCK pathway and inhibition of LIM-Kinase.

天然产物

Cat.No: T37957

Cat.No: TN1533

Target: ROCK

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