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20

抑制剂 & 化合物

25

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T1579	Mestranol Devocin,Norquen,美雌醇,Menophase	Estrogen Receptor/ERR; Estrogen/progestogen Receptor	Endocrinology/Hormones
	Mestranol (Devocin) 是一种雌激素受体激动剂，是一种非活性的前药，在转化为炔雌醇时具有生物活性。动物实验中，它可以与黄体酮联合使用，它可用于更年期激素或月经紊乱的研究。
T4058	R-IMPP	Others; Serine/threonin kinase	Cell Cycle/Checkpoint; Metabolism; Others
	R-IMPP 是抗 PCSK9分泌的药物 (IC50=4.8 μM)，靶向作用于 80S 核糖体，抑制 PCSK9 蛋白的翻译。
T40130	Nur77 modulator 1 Nur77 modulator 1	Others	Others
	Nur77 modulator 1 可与Nur77结合，KD 为 3.58 μM。它上调 Nur77 表达，介导Nur77亚细胞定位，诱导Nur77 依赖的内质网应激和自噬，可导致细胞凋亡，Nur77 modulator 1显示出抗肝癌生物活性。
T36126	TMP-153
	Acyl-CoA:cholesterol acyltransferase (ACAT) catalyses the esterification of excess cellular cholesterol with fatty acids and is important for intestinal cholesterol absorption, hepatic lipoprotein secretion, and cholesterol accumulation in vascular tissues. ACAT inhibitors improve plasma lipid profile and ameliorate proteinuria in nephrotic animals. TMP-153 is a quinolyl derivative that inhibits ACAT with IC50 values of 5-10 nM in various animals. At 0.5-1.5 mg/kg, TMP-153 dose-dependently reduc...
T10007	1,4-Chrysenequinone Chrysene-1,4-dione,1,4-屈醌	AhR	Immunology/Inflammation; Metabolism
	1,4-Chrysenequinone (Chrysene-1,4-dione) 是多环芳香烃类，是芳烃受体 (AhR) 的激活剂
T20523	Heliotrine AI3 51769,AI351769,AI3-51769,天芥菜碱
	Heliotrine leads to apoptosis of the human hepatoma cell line HepaRG.
T26394	6-Alkynyl-fucose 6-Alk-Fuc
	6-Alkynyl-fucose, a widely used fucosylation probe, acts by strongly inhibiting fucosylation and GDP-fucose synthetase FX and halting hepatoma invasion.
T26653	Arcapillin
	Arcapillin, an anticancer agent, induces apoptosis mediated at least in part by the ERS pathway and inhibits hepatoma tumor growth.
T71241	Carbovir
	Carbovir, also known as (-)-Carbovir, is a nucleoside/nucleotide reverse transcriptase inhibitor (NRTI) caused mitochondrial toxicity in human hepatoma carcinoma cell.
T37463	CAY10704
	CAY10704 is a potent inhibitor of hepatitis C virus (HCV) infection (EC50 = 17 nM) that displays low cytotoxicity of virally-infected human hepatoma Huh7.5.1 cells (CC50 = 21.3 μM). It displays good pharmacokinetics in mice when delivered intraperitoneally, with preferential liver distribution without significant hepatotoxicity. CAY10704 is selective for HCV over dengue virus (EC50 = 4.62 μM).
T11995	Melatonin-d4 N-Acetyl-5-methoxytryptamine D5,Melatonin D5,褪黑素 D5	Others	Others
	Melatonin D5, a deuterium-labeled version of melatonin, is a hormone produced by the pineal gland, known for its role as a selective ATF-6 inhibitor that promotes apoptosis in human hepatoma cells via COX-2 downregulation. Additionally, it activates melatonin receptors and exhibits antioxidative and anti-inflammatory properties.
T68588	CP-10447
	CP-10447 is an inhibitor apolipoprotein B (apoB) and triglyceride secretion in human hepatoma cells (HepG2) by inhibiting MTP activity and stimulating the early ER degradation of apoB. It is useful tool for further study of the mechanisms of apoB secretion and triglyceride-rich lipoprotein assembly.
T34582	SC-III3
	SC-III3 is a novel scopoletin derivative, induces autophagy of human hepatoma HepG2 cells through AMPK/mTOR signaling pathway by acting on mitochondria. SC-III3 reduces the viability of HepG2 cells and tumor growth of HepG2 xenograft mouse model. It induc
T74371	LEB-03-146
	LEB-03-146是一种WEE1DUBTAC（去泛素化酶靶向嵌合体），通过PEG2连接剂把AZD1775 (Adavosertib) 和OTUB1招募者EN523相连。在HEP3B肝癌细胞中，LEB-03-146能显著增强WEE1的稳定性。
T74275	LEB-03-144
	LEB-03-144 是一个 WEE1DUBTAC (去泛素化酶靶向嵌合体)，通过 C3 烷基连接剂将 AZD1775 (Adavosertib) 与 OTUB1招募者 EN523 连接起来。LEB-03-144 在 HEP3B 肝癌细胞中可显著稳定WEE1。
T35448	10-Thiastearic Acid
	Heteroatom-substituted fatty acids have been observed to modulate the extension and desaturating of fatty acids, and to influence their distribution within phospholipids pools. 10-Thiastearic acid inhibits desaturation of radiolabeled stearate to oleate in rat hepatocytes and hepatoma cells by more than 80% at a concentration of 25 μM. This activity is associated with a hypolipidemic effect, making this 10-thiastearic acid a useful tool for evaluating new anti-obesity therapeutics.
T36668	Geranylgeranoic Acid
	Geranylgeranoic acid (GGA) is an isoprenoid that has been found inS. chinensisand has anticancer activity.1It induces apoptosis in Huh7 and PLC/PRF/5 human hepatoma cells and MLE-10 transformed mouse hepatocytes, but not primary mouse hepatocytes, when used at concentrations ranging from 1 to 20 μM. GGA (10 μM) induces apoptosis in Huh7 cellsvialoss of the mitochondrial membrane potential and activation of interleukin-1β-converting enzyme (ICE) and cysteine protease precursor 32 (CPP32).2It also...
T79737	Menin-MLL inhibitor 29	Epigenetic Reader Domain	Chromatin/Epigenetic
	Menin-MLL inhibitor 29（Compound C1）是一种选择性Menin-MLLPPI抑制剂。该化合物与Menin紧密结合，具有138 nM的KD值，并以46 nM的IC50值明显抑制Menin与MBM1（Menin结合motif 1）的相互作用。在体外条件下，Menin-MLL inhibitor 29对HepG2和Hep3B肝癌细胞系表现出抑制增殖的作用（IC50s分别为0.31 μM和0.71 μM），也能有效抑制肿瘤生长。
T70313	Indoxyl Sulfate-d5 potassium salt
	Indoxyl sulfate-d5 is intended for use as an internal standard for the quantification of indoxyl sulfate by GC- or LC-MS. Indoxyl sulfate is a uremic toxin and a metabolite of tryptophan. It is formed via sulfation of indole, an intermediate generated from tryptophan by intestinal bacteria, by the sulfotransferase (SULT) isoform 1A1 variant 2 (SULT1A12) in the liver. Indoxyl sulfate activates the aryl hydrocarbon receptor (AhR) in HepG2 40/6 hepatoma* cells (EC50 = 12.1 nM in a reporter assay). ...
T35771	Destruxin B2
	Destruxin B2 is a cyclic hexadepsipeptide mycotoxin that has been found in M. anisopliae and has antiviral, insecticidal, and phytotoxic activities.1,2,3 It inhibits secretion of hepatitis B virus surface antigen (HBsAg) by Hep3B cells expressing hepatitis B virus (HBV) DNA (IC50 = 1.3 μM).1 Destruxin B2 is toxic to Sf9 insect cells in an electric cell-substrate impedance sensing (ECIS) test with a 50% inhibitory concentration (ECIS50) value of 92 μM.4 It is also phytotoxic to B. napus leaves.3 ...

化合物

Cat.No: T1579

Synonym: Devocin,Norquen,美雌醇,Menophase

Target: Estrogen Receptor/ERR, Estrogen/progestogen Receptor

Cat.No: T4058

Target: Others, Serine/threonin kinase

Nur77 modulator 1

Cat.No: T40130

Synonym: Nur77 modulator 1

Target: Others

Cat.No: T36126

1,4-Chrysenequinone

Cat.No: T10007

Synonym: Chrysene-1,4-dione,1,4-屈醌

Target: AhR

Cat.No: T20523

Synonym: AI3 51769,AI351769,AI3-51769,天芥菜碱

6-Alkynyl-fucose

Cat.No: T26394

Synonym: 6-Alk-Fuc

Cat.No: T26653

Cat.No: T71241

Cat.No: T37463

Cat.No: T11995

Synonym: N-Acetyl-5-methoxytryptamine D5,Melatonin D5,褪黑素 D5

Target: Others

Cat.No: T68588

Cat.No: T34582

Cat.No: T74371

Cat.No: T74275

10-Thiastearic Acid

Cat.No: T35448

Geranylgeranoic Acid

Cat.No: T36668

Menin-MLL inhibitor 29

Cat.No: T79737

Target: Epigenetic Reader Domain

Indoxyl Sulfate-d5 potassium salt

Cat.No: T70313

Cat.No: T35771

Cat. No.	Product Name	Target	Signaling Pathways
T5S0045	Isofraxidin 6,8-Dimethoxyumbelliferone,异秦皮啶,Phytodolor,异嗪皮啶	MMP; ERK; p38 MAPK; TLR; COX	Immunology/Inflammation; MAPK; Neuroscience; Proteases/Proteasome
	Isofraxidin (Phytodolor) 是来自刺五加的香豆素成分，抑制MMP-7表达和人肝癌细胞侵袭。它作用于肝癌细胞，抑制ERK1/2磷酸化。它减弱iNOS 和COX-2表达，还抑制TLR4/髓样分化蛋白 2 复合物的形成。
T2870	Matrine Vegard,苦参碱,Matridin-15-one,Matrinium,α-Matrine,(+)-Matrine	Mitophagy; Ferroptosis; Opioid Receptor; Autophagy	Apoptosis; Autophagy; Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	Matrine (Vegard) 是一种从槐属植物中分离出来的生物碱，可作为一种κ阿片受体激动剂，有抗肿瘤活性。
T0200	α-Lipoic Acid Thioctic acid,DL-α-Lipoic acid,(±)-α-Lipoic acid,α-硫辛酸,硫辛酸	Apoptosis; NF-κB; HIV Protease; Mitochondrial Metabolism; Endogenous Metabolite	Apoptosis; Metabolism; Microbiology/Virology; NF-κB; Proteases/Proteasome
	α-Lipoic Acid (DL-α-Lipoic acid) 是线粒体酶复合物的重要辅助因子，是一种抗氧化剂，可抑制NF-κB 依赖性的HIV-1LTR 活化。它还可诱导内质网应激介导的肝癌细胞凋亡。
T3867	Alpinetin 山姜素,(-)-alpinetin	BCL; PPAR	Apoptosis; DNA Damage/DNA Repair; Metabolism
	Alpinetin ((-)-alpinetin) 是从草豆蔻中分离得到的一种黄酮类天然产物，能够活化PPAR-γ，具有抗炎、抗菌活性。它通过抑制增殖、调节 Bcl-2 家族和 XIAP 表达、释放细胞色素 c 和激活 caspase 具有很强的抗肝癌和胰腺癌细胞作用。
T2764	(S)-10-Hydroxycamptothecin 10-羟喜树碱,10-羟基喜树碱,10-Hydroxycamptothecin,10-HCPT	Apoptosis; Topoisomerase	Apoptosis; DNA Damage/DNA Repair
	(S)-10-Hydroxycamptothecin (10-HCPT) 是一种从喜树中分离的 DNA 拓扑异构酶 I 抑制剂。它显著诱导细胞凋亡，可研究肝癌、胃癌、结肠癌和白血病。
T3810	Saikosaponin B2 柴胡皂苷 B2,柴胡皂甙 B2	Others; HCV Protease	Microbiology/Virology; Others; Proteases/Proteasome
	Saikosaponin B2 是从柴胡根中分离得到的一种活性成分，可抑制 HCV 病毒感染的侵入，有抗癌作用。
TN1600	Eclalbasaponin I	Others	Others
	Eclalbasaponin I 分离自鳢肠中，具有抗肿瘤作用，能够抑制肝癌细胞 smmc-7721 的增殖(IC50:111.1703 μg/ml)。
T2930	α-Lipoic Acid Lipoic acid,Alphalipoic acid,硫辛酸	NF-κB; HIV Protease; Mitochondrial Metabolism; Endogenous Metabolite	Metabolism; Microbiology/Virology; NF-κB; Proteases/Proteasome
	α-Lipoic Acid (Alphalipoic acid) 抑制 NF-κB 依赖性 HIV-1 LTR 活化。 α-硫辛酸诱导内质网 (ER) 应激介导的肝癌细胞凋亡。α-硫辛酸是一种抗氧化剂，是线粒体酶复合物的重要辅助因子。
T4S1999	Valepotriate 戊曲酯/缬草素,Valtrate	Apoptosis; HIV Protease	Apoptosis; Microbiology/Virology; Proteases/Proteasome
	Valepotriate (Valtrate) 是从蜘蛛香分离而来的一种天然产物，是一类新的细胞毒剂和抗肿瘤剂，对 HTC 肝癌细胞是非常有效的细胞毒剂。它可能对焦虑的精神症状具有潜在的抗焦虑作用。
T3S2344	β,β-Dimethylacrylshikonin β,β-二甲基丙烯酰紫草素,Dimethylacrylshikonin,β, β-Dimethylacrylshikonin	ERK; HIF/HIF Prolyl-Hydroxylase	Chromatin/Epigenetic; MAPK; Metabolism
	β,β-Dimethylacrylshikonin (Dimethylacrylshikonin) 是一种萘醌衍生物，从 Arnebia nobilis 中提取得到。它利用 PI3K 通路诱导 eNOS、VEGF 和 HIF-1α 的表达，促进血管生成，具有抗肿瘤活性。
T3795	Corilagin	Apoptosis; TLR; Reverse Transcriptase; Antibacterial; Autophagy	Apoptosis; Autophagy; Immunology/Inflammation; Microbiology/Virology
	Corilagin 是一种鞣酸，有抑制 RNA 肿瘤病毒逆转录酶的活性。它抑制金黄色葡萄球菌的生长，MIC 为 25 μg/mL。它有抗肿瘤活性，可用于肝癌和卵巢癌。
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。
T16160	Musk tibetene Musk tibetine	Others	Others
	Musk tibetine reveals no genotoxicity in the micronucleus test with human lymphocytes and human hepatoma cell lines. Musk tibetene is a nitro musk compound with carcinogenic activity.
TN2417	Furomollugin 5-羟基萘并[1,2-B]呋喃-4-甲酸甲酯,呋喃大叶茜草素	Antifection	Microbiology/Virology
	Furomollugin has antiviral activity, it can strongly suppress the secretion of hepatitis B surface antigen (HBsAg), with IC50 = 2.0 micrograms/mL, in human hepatoma Hep3B cells.
TN5446	Taiwanhomoflavone B
	Taiwanhomoflavone B is cytotoxic with ED(50) values of 3.8 and 3.5 microg/ml, against KB oral epidermoid carcinoma and Hepa-3B hepatoma cells, respectively.
TN4496	Marginatoxin	Caspase; Fas/FasL	Apoptosis; Proteases/Proteasome
	Marginatoxin may be a promising chemopreventive agent for treating hepatocellular carcinoma, it induces human hepatoma BEL-7402 cells apoptosis in vitro and in vivo via activation of Fas/FasL-mediated apoptotic pathway.
TN2936	3-Hydroxy-11-ursen-28,13-olide	Others	Others
	3β-Hydroxy-urs-11-en-28,13β-olide shows a potent concentration-independent cytoprotective effect against CCl4-induced injury on human hepatoma cell line relative to silymarin as a reference standard. It exhibits weak-moderate antiproliferative activity ag
TN4352	Jatamanvaltrate B	Others	Others
	Jatamanvaltrate B shows cytotoxicity against lung adenocarcinoma (A549), metastatic prostate cancer (PC-3M), colon cancer (HCT-8),and hepatoma (Bel7402) cell lines.
TN5093	Taiwanhomoflavone A	COX	Immunology/Inflammation; Neuroscience
	Taiwanhomoflavone A is cytotoxic with ED50 values of 3.4, 1.0, 2.0 and 2.5 microg/ml, respectively, against KB epidermoid carcinoma of nasopharynx, COLO-205 colon carcinoma, Hepa-3B hepatoma, and Hela cervix tumor cells.
TN3646	Chlorovaltrate K	Others	Others
	Chlorovaltrate K shows moderate cytotoxicity against lung adenocarcinoma (A 549), metastatic prostate cancer (PC-3M), colon cancer (HCT-8) and hepatoma (Bel 7402) cell lines with IC50 values of 0.89-9.76 uM.
TN5249	Volvaltrate B	Others	Others
	Volvaltrate B shows cytotoxic activity against the lung adenocarcinoma (A549), metastatic prostate cancer (PC-3M), colon cancer (HCT-8), and hepatoma (Bel7402) cell lines, with IC50 values of 8.5, 2.0, 3.2, and 6.1 uM, respectively.
TN1728	Hellebrigenin	PARP; Akt; CDK	Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
	Hellebrigenin has anti-hepatoma activities, it induces cell cycle arrest and apoptosis in human hepatocellular carcinoma HepG2 cells through inhibition of Akt. Hellebrigenin exhibites moderate to strong activity against human HL-60, SF-295, MDA-MB-435, and HCT-8 cancer cell strains without hemolysis of mouse erythrocytes.
TN4174	Guajadial	Glucokinase	Metabolism
	Guajadial shows α-glucosidase inhibitory activities significantly and its activity was better than that of Acarbose.Guajadial may act as Selective Estrogen Receptors Modulators (SERMs), therefore holding significant potential for anticancer therapy, it ex
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...
T72429	α-Lipoic Acid sodium Thioctic acid sodium,DL-α-Lipoic acid sodium,Thioctic acid sodium ; (±)-α-Lipoic acid sodium ; DL-α-Lipoic acid sodium,(±)-α-Lipoic acid sodium
	α-Lipoic Acid (Thioctic acid) sodium 是一种抗氧化剂，是线粒体酶复合物的重要辅助因子。α-Lipoic Acid sodium 可抑制NF-κB 依赖性的HIV-1LTR 活化。α-Lipoic Acid sodium 诱导内质网应激 (ERS) 介导的肝癌细胞凋亡 (apoptosis)。α-Lipoic Acid sodium 可与CPUL1 合成自组装的纳米聚合体 CPUL1-LA NA，其抗肿瘤效果优于 CPUL1。

天然产物

Cat.No: T5S0045

Synonym: 6,8-Dimethoxyumbelliferone,异秦皮啶,Phytodolor,异嗪皮啶

Target: MMP, ERK, p38 MAPK, TLR, COX

Cat.No: T2870

Synonym: Vegard,苦参碱,Matridin-15-one,Matrinium,α-Matrine,(+)-Matrine

Target: Mitophagy, Ferroptosis, Opioid Receptor, Autophagy

Cat.No: T0200

Synonym: Thioctic acid,DL-α-Lipoic acid,(±)-α-Lipoic acid,α-硫辛酸,硫辛酸

Target: Apoptosis, NF-κB, HIV Protease, Mitochondrial Metabolism, Endogenous Metabolite

Cat.No: T3867

Synonym: 山姜素,(-)-alpinetin

Target: BCL, PPAR

(S)-10-Hydroxycamptothecin

Cat.No: T2764

Synonym: 10-羟喜树碱,10-羟基喜树碱,10-Hydroxycamptothecin,10-HCPT

Target: Apoptosis, Topoisomerase

Saikosaponin B2

Cat.No: T3810

Synonym: 柴胡皂苷 B2,柴胡皂甙 B2

Target: Others, HCV Protease

Eclalbasaponin I

Cat.No: TN1600

Target: Others

Cat.No: T2930

Synonym: Lipoic acid,Alphalipoic acid,硫辛酸

Target: NF-κB, HIV Protease, Mitochondrial Metabolism, Endogenous Metabolite

Cat.No: T4S1999

Synonym: 戊曲酯/缬草素,Valtrate

Target: Apoptosis, HIV Protease

β,β-Dimethylacrylshikonin

Cat.No: T3S2344

Synonym: β,β-二甲基丙烯酰紫草素,Dimethylacrylshikonin,β, β-Dimethylacrylshikonin

Target: ERK, HIF/HIF Prolyl-Hydroxylase

Cat.No: T3795

Target: Apoptosis, TLR, Reverse Transcriptase, Antibacterial, Autophagy

Cat.No: T4S0797

Synonym: 小檗碱,Berberin,Umbellatine,黄连素

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

Cat.No: T16160

Synonym: Musk tibetine

Target: Others

Cat.No: TN2417

Synonym: 5-羟基萘并[1,2-B]呋喃-4-甲酸甲酯,呋喃大叶茜草素

Target: Antifection

Taiwanhomoflavone B

Cat.No: TN5446

Cat.No: TN4496

Target: Caspase, Fas/FasL

3-Hydroxy-11-ursen-28,13-olide

Cat.No: TN2936

Target: Others

Jatamanvaltrate B

Cat.No: TN4352

Target: Others

Taiwanhomoflavone A

Cat.No: TN5093

Target: COX

Chlorovaltrate K

Cat.No: TN3646

Target: Others

Cat.No: TN5249

Target: Others

Cat.No: TN1728

Target: PARP, Akt, CDK

Cat.No: TN4174

Target: Glucokinase

Galegine hydrochloride

Cat.No: T35532

α-Lipoic Acid sodium

Cat.No: T72429

Synonym: Thioctic acid sodium,DL-α-Lipoic acid sodium,Thioctic acid sodium ; (±)-α-Lipoic acid sodium ; DL-α-Lipoic acid sodium,(±)-α-Lipoic acid sodium

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