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23

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T9168	NSC 617145 NSC617145,NSC-617145	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	NSC 617145 (NSC617145) 是一种 WRN 解旋酶抑制剂，IC50值为 230 nM。它以浓度依赖性方式抑制 WRN 解旋酶的 ATP 酶，并诱导双链断裂和染色体异常。
T8492	BO-264	Apoptosis; FGFR	Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors
	BO-264 是一种有口服活性的转化酸性卷曲螺旋 3 抑制剂，可特异性阻断 FGFR3-TACC3融合蛋白的功能。它诱导纺锤体检查点依赖的有丝分裂阻滞，DNA 损伤和细胞凋亡，具有广谱抗肿瘤活性。
T3206	NKL 22 Histone Deacetylase Inhibitor IV,PAOA	HDAC	Chromatin/Epigenetic; DNA Damage/DNA Repair
	NKL 22 (Histone Deacetylase Inhibitor IV) 是一种有效的选择性组蛋白脱乙酰基酶(HDAC) 抑制剂，对 HDAC2/4/5/7/8 具有选择性，抑制HDAC1和HDAC3的IC50值分别为 199 和 69 nM。它可改善亨廷顿氏病转基因小鼠的疾病表型和转录异常。
T13435	TR antagonist 1	Thyroid hormone receptor(THR)	Endocrinology/Hormones
	TR antagonist 1 是一种高效甲状腺激素受体（TR）拮抗剂（对 TRα 和 TRβ 的 IC50 分别为 36 和 22 nM），可用于研究内分泌异常引起的疾病。
T74643	RSS0680	CDK; AMPK; AAK1 (AP2 associated kinase 1); PROTACs	Cell Cycle/Checkpoint; Chromatin/Epigenetic; Neuroscience; PI3K/Akt/mTOR signaling; PROTAC
	RSS0680 是一种蛋白激酶降解剂，可降解多种激酶，可用于研究激酶异常引起的疾病。
T16090	MK-0773 PF-05314882	Androgen Receptor	Endocrinology/Hormones
	MK-0773 (PF-05314882) 是一种选择性雄激素受体调节剂，能与 AR 结合（IC50：6.6 nM），可用于研究内分泌异常引起的疾病。
T22905	L748337 L-748,337	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	L748337是一种具有竞争性和高效性的 β3-肾上腺素受体拮抗剂，抑制 β3-、β2- 和 β1-肾上腺素受体发挥作用，激活 MAPK 信号传导，促进 Erk1/2 的磷酸化，抑制CL316243 的保护作用，可用于研究和β3-肾上腺素受体异常引起的疾病。
T0077	Dantrolene sodium Lapatinib ditosylate monohydrate,丹曲林钠,Dantrolene sodium salt	Others; Calcium Channel	Membrane transporter/Ion channel; Metabolism; Others
	Dantrolene sodium (Lapatinib ditosylate monohydrate) salt 是一种骨骼肌松弛药，是一种钙通道蛋白抑制剂，可抑制钙离子从肌浆释放。
T39704	KSC-34	Others	Others
	KSC-34 是蛋白二硫异构酶 A1（PDIA1）的共价修饰剂，是一种针对 PDIA1 的 a 位点的选择性抑制剂，以时间依赖的方式抑制PDIA1 还原酶活性，可用于研究淀粉样蛋白异常引起的疾病。
T38294	4-Deoxypyridoxine hydrochloride	S1P Receptor	GPCR/G Protein
	4-Deoxypyridoxine hydrochloride 通过抑制 S1P 裂解酶 (SPL) 活性来抑制细胞内 S1P 的降解，与 S1P 一样，减少化学诱导的胰岛素瘤细胞系的细胞凋亡。
T39718	Tinengotinib
	Tinengotinib, a novel compound, acts as a potent modulator of protein kinases including Aurora kinase and VEGFR kinase. With its unique properties, Tinengotinib holds promise for investigating diseases marked by abnormalities in these kinases, particularly cancer-related conditions (WO2018108079A1).
T39158	17-DMAP-GA
	17-DMAP-GA, a Geldanamycin analogue, acts as an HSP90 inhibitor, leading to cell cycle abnormalities.
T69622	Ritivixibat
	Ritivixibat为回肠胆汁酸转运蛋白(IBAT)抑制剂，同时也是胆汁酸调节剂，主要适用于心血管疾病、脂肪酸代谢及葡萄糖利用障碍、胃肠道和肝脏疾病的研究。
T40059	Nicotinamide riboside tartrate
	Nicotinamide riboside tartrate (NRT) is an oral NAD+ precursor that raises NAD+ levels, activates SIRT1 and SIRT3, and serves as a vitamin B3 (niacin) source. NRT also improves oxidative metabolism and protects against metabolic abnormalities induced by a high-fat diet. Furthermore, NRT mitigates cognitive decline in a transgenic mouse model of Alzheimer's disease.
T62791	CDK7-IN-16
	CDK7-IN-16 (compound 9) 是一种 CDK 7 的有效抑制剂 (IC50: 1-10 nM)。CDK7-IN-16 能够用于研究抗癌，特别是转录异常的癌症。
T40060	Nicotinamide riboside malate
	Nicotinamide riboside malate is an orally active NAD+ precursor that elevates NAD+ levels and stimulates the activity of SIRT1 and SIRT3. Functioning as a vitamin B3 (niacin) source, it augments oxidative metabolism and provides protection against metabolic abnormalities induced by a high-fat diet. Additionally, Nicotinamide riboside malate mitigates cognitive decline in a genetically modified mouse model of Alzheimer's disease.
T61964	RXFP3/4 agonist 2	RXFP receptor	GPCR/G Protein
	RXFP3/4 agonist 2 是一种高效的非肽双 RXFP3/4 激动剂，诱导 RXFP3 和 β-arrestin-2 之间的相互作用，可用于研究代谢异常引起的疾病。
T83870	BHD
	BHD作为一种可逆的男性避孕化合物，在体内通过(100 和 500 mg/kg)剂量引发精子生成细胞凋亡和精子管异常，破坏血-睾丸屏障，降低雄性小鼠的生育指数，效果持续两至六周。
T83328	4A7C-301
	4A7C-301是一种Nurr1激动剂，体外显示出强大的神经保护能力。在AAV2介导的α-突触核蛋白过表达雄鼠模型中，该化合物能显著纠正神经病理学异常，并改善运动及嗅觉功能障碍。此外，4A7C-301适用于帕金森病相关研究。
T80446	ω-Conotoxin FVIA	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	ω-Conotoxin FVIA为N型钙离子通道(Cav2.2)的抑制剂，具有减轻尾神经损伤大鼠模型所诱导的机械性和热性异常疼痛的作用。该化合物在开发高效且低副作用止痛药物的研究中具有潜在应用价值。
T81275	Riboxin IDP
	Riboxin (IDP) 是一种抗缺氧及抗高血压活性的口服有效嘌呤衍生物次黄苷。该化合物对心律失常也具有治疗作用，能够干预Ouabain诱导的猫、兔子、小鼠的心脏节律障碍模型。此外，Riboxin还能保护动物不受γ辐射的损害。
T70070	Cisapride tartrate
	Cisapride tartrate is chemically related to metoclopramide, but unlike metoclopramide, it does not cross the blood-brain barrier or have antidopaminergic effects. Cisapride is a serotonin-4 (5-HT4) receptor agonist. Cisapride was indicated for the symptomatic treatment of adult patients with nocturnal heartburn due to gastroesophageal reflux disease. The Food and Drug Administration (FDA) in America stopped the marketing of cisapride as of 14th July 2000. They had received at least 341 reports o...
T37631	tetranor-12(S)-HETE
	12(S)-HETE is a product of arachidonic acid metabolism through the 12-lipoxygenase pathway. It is primarily found in platelets, leukocytes, and to a lesser extent in smooth muscle cells. It enhances tumor cell adhesion to endothelial cells, fibronectin, and the subendothelial matrix. tetranor-12(S)-HETE is the major β-oxidation product resulting from peroxisomal metabolism of 12(S)-HETE in numerous tissues, and Lewis lung carcinoma cells. No biological function has yet been determined for tetran...

化合物

Cat.No: T9168

Synonym: NSC617145,NSC-617145

Target: DNA/RNA Synthesis

Cat.No: T8492

Target: Apoptosis, FGFR

Cat.No: T3206

Synonym: Histone Deacetylase Inhibitor IV,PAOA

Target: HDAC

TR antagonist 1

Cat.No: T13435

Target: Thyroid hormone receptor(THR)

Cat.No: T74643

Target: CDK, AMPK, AAK1 (AP2 associated kinase 1), PROTACs

Cat.No: T16090

Synonym: PF-05314882

Target: Androgen Receptor

Cat.No: T22905

Synonym: L-748,337

Target: Adrenergic Receptor

Dantrolene sodium

Cat.No: T0077

Synonym: Lapatinib ditosylate monohydrate,丹曲林钠,Dantrolene sodium salt

Target: Others, Calcium Channel

Cat.No: T39704

Target: Others

4-Deoxypyridoxine hydrochloride

Cat.No: T38294

Target: S1P Receptor

Cat.No: T39718

Cat.No: T39158

Cat.No: T69622

Nicotinamide riboside tartrate

Cat.No: T40059

Cat.No: T62791

Nicotinamide riboside malate

Cat.No: T40060

RXFP3/4 agonist 2

Cat.No: T61964

Target: RXFP receptor

Cat.No: T83870

Cat.No: T83328

ω-Conotoxin FVIA

Cat.No: T80446

Target: Calcium Channel

Cat.No: T81275

Synonym: IDP

Cisapride tartrate

Cat.No: T70070

tetranor-12(S)-HETE

Cat.No: T37631

Cat. No.	Product Name	Target	Signaling Pathways
T13795	Nicotinamide riboside	Sirtuin	Chromatin/Epigenetic; DNA Damage/DNA Repair
	Nicotinamide riboside 是维生素 B3 的来源，可以增强氧化代谢并防止高脂肪饮食诱导的代谢异常。它是具有口服活性的 NAD+的前体，增加 NAD+水平并激活SIRT1和SIRT3，可用于研究阿尔茨海默氏病的认知退化。
T6220	Nicotinamide riboside chloride 烟酰胺核糖氯酸盐,烟酰胺核苷	Sirtuin; Endogenous Metabolite	Chromatin/Epigenetic; DNA Damage/DNA Repair; Metabolism
	Nicotinamide riboside Chloride 是维生素 B3 的来源，可以增强氧化代谢并防止高脂肪饮食诱导的代谢异常。它是具有口服活性的 NAD+的前体，增加 NAD+水平并激活SIRT1和SIRT3，可用于研究阿尔茨海默氏病的认知退化。
T4887	3-Amino-2-methylpropanoic acid DL-3-AMINOISOBUTYRIC ACID,3-氨基异丁酸,α-Methyl-β-alanine	Endogenous Metabolite	Metabolism
	3-Amino-2-methylpropanoic acid (α-Methyl-β-alanine) 是 N-carbamyl-beta-aminoisobutyric acid 经 enzyme Beta-ureidopropionase (EC 3.5.1.6)转化后的产物，是嘧啶降解的最后一步。-尿嘧啶丙酸酶缺乏症是一种与神经异常相关的嘧啶降解的先天性错误。
T4776	Glycerol Glycerin,甘油	Endogenous Metabolite	Metabolism
	Glycerol 是甘油三酯（即脂肪和油）和磷脂的重要成分。它在食品工业中被广泛用作甜味剂和保湿剂以及药物制剂。

天然产物

Nicotinamide riboside

Cat.No: T13795

Target: Sirtuin

Nicotinamide riboside chloride

Cat.No: T6220

Synonym: 烟酰胺核糖氯酸盐,烟酰胺核苷

Target: Sirtuin, Endogenous Metabolite

3-Amino-2-methylpropanoic acid

Cat.No: T4887

Synonym: DL-3-AMINOISOBUTYRIC ACID,3-氨基异丁酸,α-Methyl-β-alanine

Target: Endogenous Metabolite

Cat.No: T4776

Synonym: Glycerin,甘油

Target: Endogenous Metabolite

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