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23

抑制剂 & 化合物

11

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T73224	AMPK-IN-1
	AMPK-IN-1 是一种 AMPK 激活剂 (对亚型α2β2γ1的 EC50为 551 nM)。AMPK-IN-1 可导致 eEF2 的 mTORC1-非依赖性磷酸化。
T73350	BAY-3827	Acyltransferase; AMPK	Chromatin/Epigenetic; Metabolism; PI3K/Akt/mTOR signaling
	BAY-3827 是一种具有强效性和选择性的 AMPK 抑制剂，具有潜在的抗肿瘤活性，在雄激素依赖性前列腺癌模型中显示出抗增殖活性。 BAY-3827 抑制乙酰 CoA 羧化酶 1 的磷酸化。
T8532	IM156	OXPHOS	Apoptosis
	IM156 (HL156A; HL271 acetate) 是衍生自二甲双胍的化合物，是一种强效的，具有口服活性的AMPK 激活剂。IM156 在动物模型中可缓解与年龄相关的认知下降。IM156 是一种有效的氧化磷酸化 (OXPHOS) 抑制剂，可用于实体肿瘤的研究。
T16342	KL1333 NQO1 activator 1	NADPH; Mitochondrial Metabolism	Metabolism
	KL1333 (NQO1 activator 1) 是口服NAD+调节剂，与 NAD(P)H: 醌氧化还原酶 1 作为底物反应。它改善线粒体脑肌病、乳酸酸中毒和中风样发作成纤维细胞的能量代谢和线粒体功能障碍。它对顺铂诱导的小鼠耳蜗培养耳毒性的保护作用。
T83125	AMPK-α1β1γ1 activator 1	AMPK	Chromatin/Epigenetic; PI3K/Akt/mTOR signaling
	AMPK-α1β1γ1激活剂1 (M1) 是一个衍生于Indole-3-carcinoma的酰基葡萄糖醛酸代谢AMPK激活剂，专一性地针对人类β1亚型，表现出38.1nM的EC50值。该化合物能够直接结合至人AMPK α1β1γ1亚型，适用于糖尿病肾病的相关研究。
T83127	AMPK activator 13	AMPK	Chromatin/Epigenetic; PI3K/Akt/mTOR signaling
	AMPK activator13作为AMPK激活剂，通过激活AMPK通路有效抑制3T3-L1细胞的有丝分裂克隆扩增，并增加细胞线粒体耗氧量，适用于肥胖研究。
T79649	CB1R/AMPK modulator 1	Cannabinoid Receptor	GPCR/G Protein
	CB1R/AMPK modulator 1 (Compound 38-S)为一种口服活性CB1R/AMPK调节剂，具有0.81 nM的Ki及3.9 nM的CB1R IC50。该化合物能够激活AMPK，且能降低食物摄入量和体重，同时改善葡萄糖耐量与胰岛素敏感性。
T79226	AMPK activator 11	Mitochondrial Metabolism	Metabolism
	AMPK activator11 是一种抗肿瘤活性纳米级化合物，有效针对多种CRC。通过激活AMPK及上调OXPHOS（mitochondrial metabolism），该化合物能选择性抑制RKO异种移植物生长，应用于肿瘤和代谢性疾病研究领域。
T78196	SIK2-IN-1
	SIK2-IN-1（化合物8g）是一种针对SIK2的高效抑制剂，在抑制其他AMPK激酶方面展现出更强的特异性。该化合物具有优良的体外ADMET属性，并显示出良好的细胞性活性。
T70296	JJO-1
	JJO-1 is a bi-quinoline that allosterically activates all AMPK αβγ isoforms in vitro except complexes containing the γ3 subunit. JJO-1 does not directly activate the autoinhibited α subunit kinase domain and differs among other known direct activators of AMPK in that allosteric activation occurs only at low ATP concentrations, and is not influenced by either mutation of the γ subunit adenylate-nucleotide binding sites or deletion of the β subunit carbohydrate-binding module.
T36535	SEC
	SEC activates ANXA7 GTPase through the AMPK/mTORC1/STAT3 signaling pathway. It selectively induces apoptosis in cancer cells expressing high levels of ITGB4 by promoting ITGB4 nuclear translocation [1][2].
T69880	YW2065
	YW2065 has excellent anti-colorectal cancer effects in vitro and in vivo. YW2065 achieves its inhibitory activity for Wnt signaling by stabilizing Axin-1, a scaffolding protein that regulates proteasome degradation of β-catenin. Simultaneously, YW2065 also led to the activation of the tumor suppressor AMPK, providing an additional anticancer mechanism. In addition, YW2065 showed favorable pharmacokinetic properties without obvious toxicity.
T74284	SH379
	SH379为2-甲基嘧啶-稠合三环二萜衍生物，是具有口服活性的有效抗迟发性性腺机能减退剂。它显著促进StAR与3β-HSD等关键睾酮合成相关酶的表达，并通过调节AMPK/mTOR信号通路刺激自噬。
T78095	Demethyleneberberine chloride	NF-κB	NF-κB
	Demethyleneberberine chloride是一种具有线粒体靶向性的天然抗氧化剂，能通过抑制NF-κB通路及调节Th细胞平衡来缓解小鼠结肠炎并抑制炎症。此外，作为一种AMPK激活剂，该化合物亦用于非酒精性脂肪性肝病（NAFLD）的研究。
T81154	SIRT1 activator 1	Sirtuin	Chromatin/Epigenetic; DNA Damage/DNA Repair
	SIRT1 activator1(compound 3)，作为海洋化合物xyloallenoide a的衍生物，最初从红树林真菌Xylaria sp中分离获得。该化合物在斑马鱼模型中展现了促进血管生成的活性，并且能够通过提升SIRT1的表达水平以及调节AMPK/Akt信号通路，来防护人类内皮祖细胞(hEPC)免受血管老化的影响。
T73125	SMTIN-T140	HSP	Cytoskeletal Signaling; Metabolism
	SMTIN-T140（化合物6a）是一种TRAP1（肿瘤坏死因子受体相关蛋白1）的高效抑制剂，IC50值为1.646 μM。该化合物表现出显著的抗癌活性，可引起线粒体功能障碍，增加线粒体ROS产生以及激活AMPK。在PC3前列腺癌细胞异种移植的小鼠模型中，SMTIN-T140有效抑制了肿瘤生长，并显示出良好的体内安全性。
T83740	Ziptide TFA
	Ziptide是多种丝氨酸/苏氨酸蛋白激酶的肽底物，包括MAPK激活蛋白激酶2（MAPKAPK2）、MAPKAPK3、MAPKAPK5、checkpoint kinase 1（Chk1）、AMP激活蛋白激酶（AMPK）和钙/钙调蛋白依赖型蛋白激酶II（CamKII）。它被用来评估CamKII活性以用于抑制剂的开发。
T76039	MOTS-c(human) acetate
	MOTS-c(human) acetate 是一种线粒体衍生的肽，可诱导 AMP 类似物AICAR 的积累，增加AMPK 的激活及其下游GLUT4的表达。MOTS-c(human) acetate 可诱导葡萄糖摄取并改善胰岛素敏感性，对肥胖，糖尿病，运动和长寿的调节具有影响。
T36106	Coumermycin A1
	Coumermycin A1 is a JAK2 signal activator. Coumermycin A1 inhibits DNA Gyrase which thereby inhibits cell division in bacteria. Coumermycin A1-induced-JAK2 signal activation increases the mRNA level of SCOS2, but reducea leptin receptor mRNA level[1]. [1]. Tiantian Zhang, et al. SOCS2 Inhibits Mitochondrial Fatty Acid Oxidation via Suppressing LepR/JAK2/AMPK Signaling Pathway in Mouse Adipocytes. Research Article.
TMIH-0181	Demethoxy Curcumin-d4
	Demethoxy Curcumin-d4 是 Demethoxy Curcumin 的氘代化合物。Demethoxy Curcumin 的 CAS 号为 22608-11-3。Demethoxycurcumin是姜黄素的主要活性成分，有抗炎和抗癌作用。
T37522	Teneligliptin
	Teneligliptin (MP-513) is a potent chemotype prolylthiazolidine-based DPP-4 inhibitor, which competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM. Teneligliptin (MP-513) inhibits all these DPP-4 enzymes in a concentration-dependent manner. The IC50s of Teneligliptin (MP-513) for rhDPP-4, human plasma, and rat plasma are 0.889, 1.75, and 1.35 nM, respectively. A study of enzyme inhibition kinetics is conducted for Teneligliptin (M...
T21693	PPM-18
	PPM-18 (NSC 73233) 是一种有效的抗炎剂，可抑制一氧化氮合酶的表达。PPM-18 是有效的 iNOS 表达抑制剂，可阻断 NF-κB 与启动子的结合。PPM-18 是维生素 K 的类似物，通过 ROS 和 AMPK 信号通路诱导膀胱癌细胞自噬和凋亡。
T36991	Monascuspiloin
	Monascuspiloin is a fungal metabolite that has been found inM. pilosusM93-fermented rice.1It induces endoplasmic reticulum stress and autophagy in PC3 prostate cancer cells. Monascuspiloin (15-45 μM) decreases viability of PC3 cells and has an additive effect on the reduction in viability of PC3 cells induced by irradiation when used at a concentration of 25 μM. It induces intratumor apoptosis and autophagy and reduces tumor growth in a PC3 mouse xenograft model when administered at doses of 40 ...

化合物

Cat.No: T73224

Cat.No: T73350

Target: Acyltransferase, AMPK

Cat.No: T8532

Target: OXPHOS

Cat.No: T16342

Synonym: NQO1 activator 1

Target: NADPH, Mitochondrial Metabolism

AMPK-α1β1γ1 activator 1

Cat.No: T83125

Target: AMPK

AMPK activator 13

Cat.No: T83127

Target: AMPK

CB1R/AMPK modulator 1

Cat.No: T79649

Target: Cannabinoid Receptor

AMPK activator 11

Cat.No: T79226

Target: Mitochondrial Metabolism

Cat.No: T78196

Cat.No: T70296

Cat.No: T36535

Cat.No: T69880

Cat.No: T74284

Demethyleneberberine chloride

Cat.No: T78095

Target: NF-κB

SIRT1 activator 1

Cat.No: T81154

Target: Sirtuin

Cat.No: T73125

Target: HSP

Cat.No: T83740

MOTS-c(human) acetate

Cat.No: T76039

Cat.No: T36106

Demethoxy Curcumin-d4

Cat.No: TMIH-0181

Cat.No: T37522

Cat.No: T21693

Cat.No: T36991

Cat. No.	Product Name	Target	Signaling Pathways
TN6751	1-HEXACOSANOL	NPC1L1; AMPK	Chromatin/Epigenetic; Membrane transporter/Ion channel; PI3K/Akt/mTOR signaling
	1-HEXACOSANOL 激活 AMPK 和肝脏自噬并抑制 SREBP2，导致降胆固醇活性和肝脏脂肪变性的改善。
T6S1683	Demethoxycurcumin Curcumin II,去甲氧基姜黄素,Desmethoxycurcumin,脱甲氧姜黄,Monodemethoxycurcumin	Apoptosis; Antioxidant; Antibacterial; Autophagy	Apoptosis; Autophagy; Microbiology/Virology; oxidation-reduction
	Demethoxycurcumin (Desmethoxycurcumin) 是姜黄素的主要活性成分，有抗炎和抗癌作用。
T5S2178	Fargesin 辛夷脂素,(+/-)-Fargesin	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Fargesin ((+/-)-Fargesin) 是一种活性新木脂素，从木兰植物中分离得到，具有抗高血压和抗炎活性。
T3S0195	Nootkatone 诺卡酮,努特卡酮,诺卡酮	AMPK	Chromatin/Epigenetic; PI3K/Akt/mTOR signaling
	Nootkatone 是一种神经保护剂，来自于Alpiniae OxyphyllaeFructus ，具有抗氧化和抗炎活性。它能够改善脂多糖诱导的阿尔茨海默氏病小鼠模型的认知障碍。
T4S0878	Prunetin 樱黄素,Prunusetin	ERK; Dehydrogenase; NF-κB	MAPK; Metabolism; NF-κB
	Prunetin (Prunusetin) 是一种O-甲基化异黄酮，具有抗炎的作用。它是人醛脱氢酶的有效抑制剂。
T4S0800	Demethyleneberberine	P450; NOS; NF-κB; HIF; AMPK	Angiogenesis; Chromatin/Epigenetic; Immunology/Inflammation; Metabolism; NF-κB; PI3K/Akt/mTOR signaling
	Demethyleneberberine 是从黄连中提取的一种天然产物，是线粒体靶向抗氧化剂。它也可作为AMPK 激活剂，用于非酒精性脂肪性肝病的研究。它通过抑制NF-κB 通路和调节 Th 细胞的平衡来减轻小鼠结肠炎并抑制炎症反应。
T6S1784	Brazilin Natural Red 24,巴西苏木素;苏枋精,Braziletto,Brasilin,Superbresiline,巴西苏木素	Apoptosis; Others; AMPK; Autophagy	Apoptosis; Autophagy; Chromatin/Epigenetic; Others; PI3K/Akt/mTOR signaling
	Brazilin (Braziletto) 是来自几种热带硬木的心材的一种红色染料前体，有软骨保护和抗炎活性。它抑制细胞增殖，促进细胞凋亡并通过 AMPK/mTOR 途径诱导自噬。
TL0014	Pinusolide	ERK; p38 MAPK; Calcium Channel; Lipoxygenase; PAFR; Caspase; JNK; AMPK	Apoptosis; Chromatin/Epigenetic; GPCR/G Protein; MAPK; Membrane transporter/Ion channel; Metabolism; PI3K/Akt/mTOR signaling; Proteases/Proteasome
	Pinusolide is a platelet activating factor ( PAF) antagonist, it may prove of therapeutic value in the treatment of hypotension, it has antileukemic potential, and could be used to treat neurodegenerative diseases. Pinusolide attenuates blockade of insulin signaling by enhancing IRS-1 tyrosine phosphorylation by the activating the AMPK pathway, indicates the targeting of AMPK represents a new therapeutic strategy for hyperglycemia-induced insulin resistance and type 2 diabetes.
T79949	Foenumoside B	PPAR	DNA Damage/DNA Repair; Metabolism
	Foenumoside B为从Lysimachia foenum-graecum中提取的三萜皂苷。该化合物通过激活AMPK信号传导和抑制PPARγ诱导的脂肪生成，调节脂质代谢向脂肪分解方向转变。因其调控作用，Foenumoside B常用于研究肥胖及相关代谢疾病。
T35532	Galegine hydrochloride
	Galegine hydrochloride, a guanidine derivative derived from G. officinalis, plays a role in inducing weight loss in mice and has contributed to the development of biguanides, including metformin and phenformin. This compound stimulates AMPK activation in 3T3-L1 adipocytes, L6 myotubes, H4IIE rat hepatoma, and HEK293 human kidney cell lines. Additionally, galegine hydrochloride exhibits antibacterial properties, particularly demonstrating a minimum inhibitory concentration of 4 mg/L against Staph...
T35624	Ajoene
	Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities, including antibacterial, anticancer, antiplatelet, and antioxidant properties.1,2,3,4It is active against Gram-positive (MICs = 5-160 &#181g/ml) and Gram-negative bacteria (MICs = 136-200 &#181g/ml), as well as yeasts (MICs = 10-20 &#181g/ml).1Ajoene is cytotoxic to mouse melanoma cells (IC50= 18 &#181M), as well as human colon, lung, mammary, and pancreatic cancer cells (IC50s = 7-41 &#181M).2It reduces...

天然产物

Cat.No: TN6751

Target: NPC1L1, AMPK

Demethoxycurcumin

Cat.No: T6S1683

Synonym: Curcumin II,去甲氧基姜黄素,Desmethoxycurcumin,脱甲氧姜黄,Monodemethoxycurcumin

Target: Apoptosis, Antioxidant, Antibacterial, Autophagy

Cat.No: T5S2178

Synonym: 辛夷脂素,(+/-)-Fargesin

Target: Adrenergic Receptor

Cat.No: T3S0195

Synonym: 诺卡酮,努特卡酮,诺卡酮

Target: AMPK

Cat.No: T4S0878

Synonym: 樱黄素,Prunusetin

Target: ERK, Dehydrogenase, NF-κB

Demethyleneberberine

Cat.No: T4S0800

Target: P450, NOS, NF-κB, HIF, AMPK

Cat.No: T6S1784

Synonym: Natural Red 24,巴西苏木素;苏枋精,Braziletto,Brasilin,Superbresiline,巴西苏木素

Target: Apoptosis, Others, AMPK, Autophagy

Cat.No: TL0014

Target: ERK, p38 MAPK, Calcium Channel, Lipoxygenase, PAFR, Caspase, JNK, AMPK

Cat.No: T79949

Target: PPAR

Galegine hydrochloride

Cat.No: T35532

Cat.No: T35624

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