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Search Results for " cancer metabolism "

34

抑制剂 & 化合物

12

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T6816	DASA-58	PKM	Metabolism
	DASA58 是一种有效的丙酮酸激酶M2 (PKM2) 活化剂，其中AC90=680 nM，AC50=38 nM。
T3713	BAY-876	transporter	Metabolism
	BAY-876 是口服有效的，选择性的葡萄糖转运蛋白 1 (GLUT1) 抑制剂（IC50= 2 nM）。BAY-876 对 GLUT1 选择性比 GLUT2，GLUT3 和 GLUT4 高（>130 倍）。BAY-876 对糖酵解代谢和卵巢癌生长也有有效的抑制作用。
T7835	CM10 CM 10	Dehydrogenase	Metabolism
	CM10是一种有效的乙醛脱氢酶 1A (ALDH1A) 家族选择性抑制剂，对于 ALDH1A1，ALDH1A2 和 ALDH1A3 的IC50分别为 1700、740 和 640 nM。CM 10 可以调节新陈代谢并具有抗癌活性。
T8500	VLX600	OXPHOS; Mitochondrial Metabolism; Autophagy	Apoptosis; Autophagy; Metabolism
	VLX600 是一种铁螯合氧化磷酸化抑制剂，是一种细胞渗透性抗癌剂。它通过减少肿瘤细胞中的线粒体氧化磷酸化起作用。
T8308	NL-1	Mitochondrial Metabolism; Autophagy	Autophagy; Metabolism
	NL-1 是一种mitoNEET 抑制剂，具有抗白血病作用。它抑制 REH 和 REH/Ara-C 细胞生长，IC50分别为 47.35 µM 和 56.26 µM。
T6157	Devimistat CPI-613,辛酸,CPI613,CPI 613,6,8-Bis(benzylthio)octanoic acid	Apoptosis; Dehydrogenase; Mitochondrial Metabolism	Apoptosis; Metabolism
	Devimistat (6,8-Bis(benzylthio)octanoic acid) 是一种线粒体代谢抑制剂，还是一种lipoic acid 拮抗剂，能阻断线粒体能量代谢，诱导多种癌细胞凋亡。
T9211	Mito-LND Mito-Loidamine	OXPHOS; Reactive Oxygen Species; Mitochondrial Metabolism; Autophagy	Apoptosis; Autophagy; Immunology/Inflammation; Metabolism; NF-κB
	Mito-LND (Mito-Loidamine) 是一种有口服活性和靶向线粒体的氧化磷酸化抑制剂。它抑制线粒体生物能，刺激活性氧的形成，并诱导肺癌细胞自噬细胞死亡。
T8766	GOT1 inhibitor-1 GOT1 inhibitor 2c	Others	Others
	GOT1 inhibitor-1 (GOT1 inhibitor 2c) 是一种新型的、非共价的谷氨酸草酰乙酸转氨酶 1 (GOT1) 抑制剂(IC50:8.2 uM)，是一种戊酸衍生物。它可用于以及胰腺导管腺癌 (PDAC) 。
T35343	MTI-31 MTI-31,LXI-15029	mTOR	PI3K/Akt/mTOR signaling
	MTI-31 (LXI-15029) 是口服有效的，高度选择性的mTORC1和mTORC2抑制剂，对 mTOR 的Kd 为 0.20 nM，IC50为 39 nM。MTI-31可用于乳腺癌的研究。
T13748	L-2-Hydroxyglutaric acid disodium S-2-羟基戊二酸,(S)-2-Hydroxyglutaric acid disodium	Histone Demethylase; Mitochondrial Metabolism	Chromatin/Epigenetic; Metabolism
	L-2-Hydroxyglutaric acid disodium ((S)-2-Hydroxyglutaric acid disodium) 是一种表观遗传修饰因子，是肾癌中的表观遗传修饰剂和推定的癌代谢物，可用于肾癌的相关研究。它抑制线粒体肌酸激酶活性，Km 和 Ki 分别为 2.52 mM 和11.13 mM。它可抑制组蛋白去甲基化酶，从而促进组蛋白甲基化。
T27259	Emitefur BOFA2,BOF A2,BOF-A2	Others	Others
	Emitefur (BOF-A 2)是一种有口服活性和有效性的 5-氟尿嘧啶衍生物，具有抗癌和抗肿瘤活性。Emitefur 可用于研究晚期胃癌、乳腺癌和代谢相关疾病。
T9768L	Ninerafaxstat trihydrochloride Ninerafaxstat trihydrochloride(2254741-41-6 Free base)	Others	Others
	Ninerafaxstat trihydrochloride 将细胞代谢由脂肪酸氧化转变为葡萄糖氧化。 Ninerafaxstat trihydrochloride 改善整体线粒体呼吸并减少脂肪酸氧化，从而抑制癌细胞的增殖和生长。
T37986	D-Mannose-6-Phosphate sodium salt hydrate	Others	Others
	D-Mannose-6-Phosphate sodium salt hydrate 是一种多功能单糖，可用于研究代谢、溶酶体传递和癌症。
T77552	SLU-PP-1072	Apoptosis; Estrogen/progestogen Receptor	Apoptosis; Endocrinology/Hormones
	SLU-PP-1072 是一种 ERRα和ERRγ 反向双重激动剂，破坏 PCa 细胞代谢，通过细胞周期失调诱导凋亡 (apoptosis)。SLU-PP-1072 用于研究前列腺癌 (PCa) 。
T60839	SLMP53-1	p53	Apoptosis
	SLMP53-1 是一种 p53 激活剂，具有抗肿瘤活性，抑制 wt 和 mutp53，激活异种移植人肿瘤组织中葡萄糖代谢的重编程，干扰血管生成和迁移。SLMP53-1 抑制肿瘤细胞生长，可用于研究人直肠癌。
T17224	VER-246608	Dehydrogenase; PDK	Metabolism; PI3K/Akt/mTOR signaling
	VER-246608 是ATP 竞争性的丙酮酸脱氢酶激酶抑制剂，对PDK-1，PDK-3，PDK-2，和PDK-4的IC50分别为 35 nM，40 nM，84 nM 和 91 nM。
T27417L	Glutathione arsenoxide hydrochloride GSAO HCl,Glutathione arsenoxide hydrochloride(1271726-51-2 Free base)	Apoptosis; AChR	Apoptosis; Neuroscience
	Glutathione arsenoxide hydrochloride (Glutathione arsenoxide hydrochloride(1271726-51-2 Free base)) 是一种潜在的抗癌活性分子和肿瘤代谢抑制剂。Glutathione arsenoxide hydrochloride 靶向线粒体内膜腺嘌呤核苷酸转移酶 (ANT)，对细胞增殖有抑制作用，促进细胞凋亡。Glutathione arsenoxide hydrochloride 可用于识别如蛋白质二硫异构酶一样的细胞表面蛋白质。
T67831	HIF-2α agonist 2	HIF/HIF Prolyl-Hydroxylase; HIF	Angiogenesis; Chromatin/Epigenetic; Metabolism
	HIF-2α agonist 2 是一种 HIF-2α 激动剂，对HIF-2α的EC50 值为 1.68 μM。HIF-2α agonist 2可以促进HIF-2a-ARNT 复合物3z 结构中ARNT A/B 环的稳定性，对 786-O-HRE-Luc 细胞无细胞毒性。HIF-2α agonist 2可用于氧代谢研究，与癌症的发生密切相关。
T33392	MIP-1095 I-123 123-I-MIP-1095,(123I)MIP 1095
	MIP-1095 I-123, as a radiotracer, is under investigation in clinical trial NCT00712829 (Evaluating the Safety, Pharmacokinetics, Tissue Distribution, Metabolism and Dosimetry of Two Prostate Cancer Imaging Agents).
T72693	PKM2 activator 5	PKM	Metabolism
	PKM2 activator 5 是一种新型有效的 PKM2 激活剂（ AC50：0.316 µM），具有潜在的抗癌活性，可用于研究癌症代谢相关疾病。
T9768	Ninerafaxstat	Others	Others
	Ninerafaxstat 可以将细胞代谢从脂肪酸氧化转变为葡萄糖氧化，降低脂肪酸氧化，改善线粒体呼吸。
T12003	Mensacarcin	Others	Others
	Mensacarcin, a highly complex polyketide compound, exhibits multifaceted effects on cellular processes. Specifically, it targets mitochondria, perturbs energy metabolism within these organelles, and activates caspase-dependent apoptotic pathways. Functionally, Mensacarcin can serve as a cytotoxic constituent in antibody-drug conjugates (ADCs). Furthermore, this antibiotic compound displays broad-spectrum inhibition of cell growth across various cancer cell lines and demonstrates potent induction...
T35874	CC260
	CC260 is a selective PI5P4Kα and PI5P4Kβ inhibitor with Kis of 40 nM and 30 nM, respectively. CC260 does not inhibit or weakly inhibits other protein kinases, such as Plk1 and RSK2. CC260 can be used for cell energy metabolism, diabetes and cancer research[1]. In cultured C2C12 myotubes, CC260 (20 μM) enhances Insulin-induced Akt phosphorylation at both Thr-308 and Ser-473 but suppresses S6K phosphorylation (Thr-389) by mTORC1[1]. CC260 (2.5 μM, 5 μM, 10 μM, 20 μM) significantly increases phosph...
T74279	Curcumin monoglucuronide
	Curcumin monoglucuronide 被称为葡糖醛酸结合物，是姜黄素的体内代谢产物之一。Curcumin monoglucuronide 用于研究姜黄素的代谢及其作为活性分子的开发。Curcumin monoglucuronide 具有研究癌症疾病的潜力。
T81743	mTORC1-IN-1	mTOR	PI3K/Akt/mTOR signaling
	mTORC1-IN-1（compound T1）为一种rapalog及选择性mTORC1抑制剂，调节细胞生长和代谢，与多种疾病如癌症相关。该化合物通过与FKBP12-FRB复合物结合（对接分数−11.6 kcal/mol）来靶向mTORC1。
T79783	NSC 48160	Apoptosis	Apoptosis
	NSC 48160对胰腺癌细胞具有抑制作用，IC50分别针对CPFAC-1为84.3μM，对BxPC-3为94.5μM。此外，NSC 48160能够诱导胰腺癌细胞(apoptosis)。该化合物亦能改善代谢综合征症状，包括NASH、肥胖及脂质代谢紊乱。
T22552	AD57 (hydrochloride)	Others	Others
	AD57, as polypharmacological cancer therapeutic, is designed to regulate multiple targets related to cancer blocks the receptor tyrosine kinase RET in Drosophila (IC50: 2 nM). AD57 effectively suppresses tyrosine kinase RET, weakens the activity of numero
T78208	Leramistat HMC-C-01-A,MBS2320	Mitochondrial Metabolism	Metabolism
	Leramistat (HMC-C-01-A; MBS2320)为线粒体复合物1抑制剂，关与调控细胞代谢及免疫代谢。该化合物被用于抑制诸如特应性皮炎的皮肤病、自身免疫性与炎症性疾病和癌症，以及破骨细胞介导的疾病。
T40565	5MPN
	5MPN is a novel compound that functions as a highly potent and selective inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 4 (PFKFB4). This compound demonstrates oral activity and serves as a first-in-class inhibitor. Through competitive inhibition of the F6P binding site, 5MPN effectively hinders the functionality of PFKFB4, with a Ki value of 8.6 μM. Importantly, it exhibits no inhibitory effects on PFK-1 or PFKFB3. By specifically targeting the sugar metabolism of tumors, 5MPN...
T69685	AGPS-IN-2i	MMP	Proteases/Proteasome
	AGPS-IN-2i 是一种高效且具有很高亲和力的烷基甘油磷酸酯合成酶抑制剂的，可控制着细胞中醚脂的利用和代谢，降低了醚类脂质水平和细胞迁移率，促进癌细胞的增殖和运动。AGPS-IN-2i 在 PC-3和 MDA-MB-231癌细胞中测试时通过调节 E-cadherin、Snail 和 MMP2的表达水平，特异性地损害了上皮向间质转化（EMT）。AGPS-IN-2i 对癌细胞增殖具有抑制作用。
T60510	Perhexiline
	Perhexiline 是一种口服活性的 CPT1和 CPT2抑制剂，可降低脂肪酸的代谢。Perhexiline 可以穿过血脑屏障 (BBB)具有抗癌活性。Perhexiline 诱导肝细胞中的线粒体功能障碍和细胞凋亡。因此，Perhexiline 可用于研究癌症和心绞痛等心血管疾病。
T37355	CAY10703
	Dichloroacetate (DCA) is an inhibitor of all pyruvate dehydrogenase kinase (PDHK) isoforms, which are enzymes that phosphorylate and inhibit PDH in mitochondria. Inhibition of PDHK shifts cell metabolism from glycolysis to mitochondrial glucose oxidation, an effect that has relevance to cancer, type 2 diabetes, and other diseases. CAY10703 is a DCA trimer that is at least 10-fold more cytotoxic against leukemia cell lines than DCA. It is approximately 3-fold less cytotoxic than DCA against perip...
T35676	17β-hydroxy Exemestane
	17β-hydroxy Exemestane is the primary active metabolite of exemestane . It is formed by metabolism of exemestane by the cytochrome P450 (CYP) isoforms CYP1A and CYP4A11. 17β-hydroxy Exemestane is an aromatase inhibitor (IC50 = 69 nM using human placental microsomes) and an androgen receptor (AR) agonist (IC50 = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC50 = 21.2 μM). It stimulates growth of AR- and ERα-positive MCF-7 (EC50 = 2.7 μM) and T47D breast cancer cells (EC50s = ...
T36807	Estradiol 17-(β-D-Glucuronide) (sodium salt hydrate)
	Estradiol 17-(β-D-glucuronide) (E217G) is an estrogen metabolite formed in the liver and subsequently excreted in bile.1It acts as a substrate of the multidrug resistance protein 2 (MRP2; Km= 75 μM), and through MRP2-mediated transport, functions as a cholestatic agent, decreasing bile flow.1,2In addition to binding to the MRP2 transport site, E217G has been shown to bind to an allosteric site that through positive cooperativity activates its own transportviaMRP2 and the transport of other MRP2 ...

化合物

Cat.No: T6816

Target: PKM

Cat.No: T3713

Target: transporter

Cat.No: T7835

Synonym: CM 10

Target: Dehydrogenase

Cat.No: T8500

Target: OXPHOS, Mitochondrial Metabolism, Autophagy

Cat.No: T8308

Target: Mitochondrial Metabolism, Autophagy

Cat.No: T6157

Synonym: CPI-613,辛酸,CPI613,CPI 613,6,8-Bis(benzylthio)octanoic acid

Target: Apoptosis, Dehydrogenase, Mitochondrial Metabolism

Cat.No: T9211

Synonym: Mito-Loidamine

Target: OXPHOS, Reactive Oxygen Species, Mitochondrial Metabolism, Autophagy

GOT1 inhibitor-1

Cat.No: T8766

Synonym: GOT1 inhibitor 2c

Target: Others

Cat.No: T35343

Synonym: MTI-31,LXI-15029

Target: mTOR

L-2-Hydroxyglutaric acid disodium

Cat.No: T13748

Synonym: S-2-羟基戊二酸,(S)-2-Hydroxyglutaric acid disodium

Target: Histone Demethylase, Mitochondrial Metabolism

Cat.No: T27259

Synonym: BOFA2,BOF A2,BOF-A2

Target: Others

Ninerafaxstat trihydrochloride

Cat.No: T9768L

Synonym: Ninerafaxstat trihydrochloride(2254741-41-6 Free base)

Target: Others

D-Mannose-6-Phosphate sodium salt hydrate

Cat.No: T37986

Target: Others

Cat.No: T77552

Target: Apoptosis, Estrogen/progestogen Receptor

Cat.No: T60839

Target: p53

Cat.No: T17224

Target: Dehydrogenase, PDK

Glutathione arsenoxide hydrochloride

Cat.No: T27417L

Synonym: GSAO HCl,Glutathione arsenoxide hydrochloride(1271726-51-2 Free base)

Target: Apoptosis, AChR

HIF-2α agonist 2

Cat.No: T67831

Target: HIF/HIF Prolyl-Hydroxylase, HIF

Cat.No: T33392

Synonym: 123-I-MIP-1095,(123I)MIP 1095

PKM2 activator 5

Cat.No: T72693

Target: PKM

Cat.No: T9768

Target: Others

Cat.No: T12003

Target: Others

Cat.No: T35874

Curcumin monoglucuronide

Cat.No: T74279

Cat.No: T81743

Target: mTOR

Cat.No: T79783

Target: Apoptosis

AD57 (hydrochloride)

Cat.No: T22552

Target: Others

Cat.No: T78208

Synonym: HMC-C-01-A,MBS2320

Target: Mitochondrial Metabolism

Cat.No: T40565

Cat.No: T69685

Target: MMP

Cat.No: T60510

Cat.No: T37355

17β-hydroxy Exemestane

Cat.No: T35676

Estradiol 17-(β-D-Glucuronide) (sodium salt hydrate)

Cat.No: T36807

Cat. No.	Product Name	Target	Signaling Pathways
T2899	Liquiritin Liquiritigenin-4'-O-glucoside,Liquiritoside,甘草苷	Reactive Oxygen Species	Immunology/Inflammation; Metabolism; NF-κB
	Liquiritin (Liquiritigenin-4'-O-glucoside) 是一种从甘草中分离出的类黄酮，是一种竞争性的 AKR1C1 抑制剂，对 AKR1C1，AKR1C2 和 AKR1C3 的 IC50分别为 0.62 μM，0.61 μM 和 3.72 μM，在体内有效抑制 AKR1C1 介导的孕酮代谢。它是一种抗氧化剂，具有神经保护、抗癌、抗炎的活性。
T9352	hydrocotarnine	Others	Others
	hydrocotarnine 是 Cbl 的抑制剂。
T2966	Beta-Sitosterol Cupreol,谷甾醇,Beta-Sitosterol,β-Sitosterol,Azuprostat,SKF 14463,beta-谷甾醇,22,23-Dihydrostigmasterol,Betaprost	Apoptosis; Lipase; Endogenous Metabolite	Apoptosis; Metabolism
	Beta-Sitosterol (SKF 14463) 是一种植物甾醇，干扰细胞周期、细胞凋亡、增殖、存活、侵袭、血管生成和炎症等多种细胞信号通路。
T7032	Eupatorin	Others; P450	Metabolism; Others
	Eupatorin 是天然存在的黄酮，可捕获 G2-M 细胞周期，激活多个 caspase、细胞色素 C 的释放、多聚 (ADP-核糖) 聚合酶的裂解，促使凋亡细胞死亡。
T6S0119	Dauricine 蝙蝠葛碱	Apoptosis; Others; NF-κB	Apoptosis; NF-κB; Others
	Dauricine 是存在于北豆根粉末中的一种双苯异喹啉生物碱，具有抗炎活性。它通过抑制NF-κB 激活，剂量依赖性地抑制结肠癌细胞的增值和侵袭，并诱导凋亡。
T6491	(-)-(S)-Equol (−)-Equol,Equol,4',7-Dihydroxyisoflavan,4',7-Isoflavandiol,雌马酚	Estrogen Receptor/ERR; Estrogen/progestogen Receptor; Endogenous Metabolite	Endocrinology/Hormones; Metabolism
	(-)-(S)-Equol (4',7-Dihydroxyisoflavan) 是雌激素受体β的高亲和力配体。
T4000	(±)-Equol Equol,(±)-雌马酚,(R,S)-Equol	Estrogen Receptor/ERR; Estrogen/progestogen Receptor; Drug Metabolite	Endocrinology/Hormones; Metabolism
	(±)-Equol ((R,S)-Equol) 是 equol 的外消旋体。它对 ERα 和 ERβ 的 EC50s of 分别为 200 和 74 nM。Equol 是大豆异黄酮黄豆苷和大豆黄素的代谢产物。
T37984	D-Fructose-1,6-bisphosphate sodium salt hydrate	Others	Others
	D-Fructose-1,6-bisphosphate sodium salt hydrate 是碳水化合物代谢的中间体，包括糖酵解和糖异生。在糖酵解过程中，它是由磷酸果糖激酶磷酸化果糖-6-磷酸产生的。由果糖-1,6-二磷酸酶-1介导的逆反应是糖异生的限速步骤之一。同样的反应也发生在植物的叶绿体中，D-Fructose-1,6-bisphosphate sodium salt hydrate 作为还原性戊糖磷酸循环的一部分。由于癌细胞采用糖酵解作为代谢能量产生的主要来源，这一途径已成为癌症化疗的主要靶点。
T4S0797	Berberine 小檗碱,Berberin,Umbellatine,黄连素	Reactive Oxygen Species; Topoisomerase; Endogenous Metabolite; Antibacterial; Antibiotic; Autophagy	Autophagy; DNA Damage/DNA Repair; Immunology/Inflammation; Metabolism; Microbiology/Virology; NF-κB
	Berberine (Umbellatine) 是从中草药黄连中分离出来的一种生物碱抗生素。它诱导活性氧生成并抑制 DNA 拓扑异构酶，具有抗肿瘤特性。
T4S2126	Ginkgetin 银杏双黄酮,银杏素	Apoptosis; Wnt/beta-catenin; COX; STAT; Autophagy	Apoptosis; Autophagy; Cytoskeletal Signaling; Immunology/Inflammation; JAK/STAT signaling; Neuroscience; Stem Cells
	Ginkgetin 是从银杏叶中分离得到的一种双黄酮，具有抗肿瘤、抗炎、神经保护、抗真菌的作用。它也是 Wnt 信号抑制剂，IC50值为 5.92 μM。
T3824	Jaceosidin	Apoptosis; BCL; COX; UGT	Apoptosis; Immunology/Inflammation; Metabolism; Neuroscience
	Jaceosidin 是从毛莲蒿中得到的一种黄酮类天然产物，可激活Bax，下调 Mcl-1 和 c-FLIP 的表达，诱导癌细胞凋亡。它能够降低炎性因子水平，激活 NF-κB，抑制COX-2的表达，具有抗癌和抗炎作用。
T36179	Aspulvinone O
	Aspulvinone O is a fungal metabolite that has been found in P. variotti and has antioxidant and anticancer activities.1,2 It scavenges 2,2-diphenyl-1-picrylhydrazyl radicals in a cell-free assay (IC50 = 11.6 μM).1 Aspulvinone O inhibits aspartate transaminase 1 (GOT1; Kd = 3.32 μM) and is cytotoxic to PANC-1, AsPC-1, and SW1990 pancreatic cancer cells (IC50s = 20.54-26.8 μM).2 It reduces the oxygen consumption rate (OCR) and induces apoptosis in SW1990 cells. Aspulvinone O (2.5 and 5 mg/kg) redu...

天然产物

Cat.No: T2899

Synonym: Liquiritigenin-4'-O-glucoside,Liquiritoside,甘草苷

Target: Reactive Oxygen Species

Cat.No: T9352

Target: Others

Beta-Sitosterol

Cat.No: T2966

Synonym: Cupreol,谷甾醇,Beta-Sitosterol,β-Sitosterol,Azuprostat,SKF 14463,beta-谷甾醇,22,23-Dihydrostigmasterol,Betaprost

Target: Apoptosis, Lipase, Endogenous Metabolite

Cat.No: T7032

Target: Others, P450

Cat.No: T6S0119

Synonym: 蝙蝠葛碱

Target: Apoptosis, Others, NF-κB

Cat.No: T6491

Synonym: (−)-Equol,Equol,4',7-Dihydroxyisoflavan,4',7-Isoflavandiol,雌马酚

Target: Estrogen Receptor/ERR, Estrogen/progestogen Receptor, Endogenous Metabolite

Cat.No: T4000

Synonym: Equol,(±)-雌马酚,(R,S)-Equol

Target: Estrogen Receptor/ERR, Estrogen/progestogen Receptor, Drug Metabolite

D-Fructose-1,6-bisphosphate sodium salt hydrate

Cat.No: T37984

Target: Others

Cat.No: T4S0797

Synonym: 小檗碱,Berberin,Umbellatine,黄连素

Target: Reactive Oxygen Species, Topoisomerase, Endogenous Metabolite, Antibacterial, Antibiotic, Autophagy

Cat.No: T4S2126

Synonym: 银杏双黄酮,银杏素

Target: Apoptosis, Wnt/beta-catenin, COX, STAT, Autophagy

Cat.No: T3824

Target: Apoptosis, BCL, COX, UGT

Cat.No: T36179

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