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20

抑制剂 & 化合物

8

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T9945	MNK8 3-methyl-6-(naphthalen-1-yl)pyrimidine-2,4(1H,3H)-dione	STAT	JAK/STAT signaling; Stem Cells
	MNK8 (3-methyl-6-(naphthalen-1-yl)pyrimidine-2,4(1H,3H)-dione) 是一种有效的STAT3抑制剂，降低STAT3与DNA 结合的能力，对肝癌细胞也有良好的生长抑制作用。
T1406	Amantadine hydrochloride 盐酸金刚烷胺,1-adamantanamine HCl,1-Adamantanamine hydrochloride,Symmetrel,CI-719,Amantadine HCl,1-Adamantylamine hydrochloride	Dopamine Receptor; Influenza Virus	GPCR/G Protein; Microbiology/Virology; Neuroscience
	Amantadine hydrochloride (CI-719) 是一种抗病毒药物，用于预防或对症治疗甲型流感和帕金森病。它阻断质子流通过 M2 离子通道，从而阻止病毒 RNA 释放到感染细胞的细胞质中。
T60420	Anticancer agent 73	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	Anticancer agent 73 是一种抗癌剂，它能有效地靶向反式激活反应（TAR）RNA 结合蛋白2（TRBP），并破坏TRBP-Dicer 的相互作用。Anticancer agent 73 通过调节 HCC 细胞中 miRNA 组和蛋白质组的表达谱，在体外和体内抑制 HCC 的生长和转移。
T60604	XST-14	Apoptosis; Autophagy	Apoptosis; Autophagy
	XST-14 是一种具有竞争性和特异性的 ULK1 抑制剂（IC50: 26.6 nM）。XST-14 通过抑制ULK1 下游底物的磷酸化来阻断自噬。XST-14 诱导细胞凋亡并抑制 HCC 细胞的生长。
T64529	MDL-800 MDL 800,MDL800	Sirtuin	Chromatin/Epigenetic; DNA Damage/DNA Repair
	SIRT6, responsible for deacetylation of histone H3 Nε-acetyl-lysines 9 (H3K9ac) and 56 (H3K56ac), is a tumor suppressor which has frequently been found to have low expression in various cancers. MDL-800 is a selective SIRT6 activator. It increased the deacetylase activity of SIRT6 by up to 22-fold and led to a global decrease in H3K9ac and H3K56ac levels in human hepatocellular carcinoma (HCC) cells. Also, it inhibited the proliferation of HCC cells via SIRT6-driven cell-cycle arrest and was eff...
T3226	Paritaprevir ABT-450,Veruprevir,帕利瑞韦	HCV Protease	Microbiology/Virology; Proteases/Proteasome
	Paritaprevir (ABT-450) 是一种口服生物可利用的合成酰基磺酰胺抑制剂，可抑制丙型肝炎病毒 (HCV) 蛋白酶复合物，由非结构蛋白 3 和 4A (NS3/NS4A) 组成，对 HCV 基因型 1 具有潜在活性。给药后，paritaprevir 可逆地结合 HCV NS3/NS4A 蛋白酶的活性中心和结合位点，并阻止 NS3/NS4A 蛋白酶介导的多蛋白成熟。这会破坏病毒蛋白的加工和病毒复制复合物的形成，从而抑制病毒在 HCV 基因型 1 感染的宿主细胞中的复制。 NS3 是一种丝氨酸蛋白酶，对于 HCV 多蛋白内多个位点的蛋白水解切割至关重要，并且在 HCV 核糖核酸 (RNA) 复制过程中起关键作用。 NS4A 是 NS3 的激活因子。 HCV 是属于黄病毒科的一种小的、有包膜的单链 RNA 病毒，感染与肝细胞癌 (HCC) 的发展有关。
T15234	ENMD-1198 IRC 110160,ENMD-119,ENMD 1198	HIF; STAT	Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells
	ENMD-119 is a 2-methoxyestradiol analog with antiproliferative and antiangiogenic activity. It is suitable for inhibiting HIF-1α and STAT3 in human HCC cells.
T38977	Autophagy-IN-C1 Autophagy-IN-C1
	Autophagy-IN-C1是一种含有尿素的金鸡纳生物碱衍生物。Autophagy-IN-C1 不仅诱导肝细胞癌（HCC）细胞凋亡，而且阻断自噬。
T68875	Xylocydine
	Xylocydine is a novel Cdk inhibitor, which is an effective inducer of apoptosis in hepatocellular carcinoma cells in vitro and in vivo. Xylocydine also strongly inhibits the activity of Cdk7 and Cdk9, in vitro as well as in cell cultures, that is temporally associated with apoptotic cell death in xylocydine-induced HCC cells. Xylocydine can effectively suppress the growth of HCC xenografts in Balb/C-nude mice by preferentially inducing apoptosis in the xenografts, whereas the drug did not cause...
T70988	Ibulocydine
	Ibulocydine is a potent CDK inhibitor. Ibulocydine has high activity against Cdk7/cyclin H/Mat1 and Cdk9/cyclin T. Ibulocydine inhibited the growth of HCC cells more effectively than other Cdk inhibitors, including olomoucine and roscovitine, whereas ibulocydine as well as the other Cdk inhibitors and BMK-Y101 minimally influenced the growth of normal hepatocyte cells. Ibulocydine induced apoptosis in HCC cells, most likely by inhibiting Cdk7 and Cdk9. In vitro treatment of HCC cells with ibuloc...
T64085	KRAS G12C inhibitor 43
	KRAS G12C inhibitor 43 是 KRAS G12C 的有效抑制剂，能够抑制 H358 细胞 (IC50: 0.001-1 μM μM)、 A549 细胞 (IC50>1 μM)、 HCC 细胞 (IC50>1 μM) 的迁移和增殖。
T62704	HBV-IN-23
	HBV-IN-23 (Compound 5k) 是一种 HBV DNA 复制抑制剂 (IC50: 0.58 μM)。HBV-IN-23 能够抑制药物敏感和耐药株。HBV-IN-23 可以诱导 HepG2 细胞凋亡，表现出抗肝癌细胞 (HCC) 效果。
T79341	Tubulin polymerization-IN-45
	Tubulin polymerization-IN-45 是针对微管蛋白的靶向抑制剂，通过与微管蛋白秋水仙碱结合位点相结合，能够诱导肝细胞癌细胞 (HCC) 发生细胞凋亡 (apoptosis)。
T74225	ROS-ERS inducer 1
	ROS-ERS inducer 1 是一种基于4,5-二芳基咪唑的Pt(II)-N-杂环卡宾 (Pt(II)-NHC) 复合物，属于 II 型免疫原性细胞死亡(ICD)诱导剂。它能促使内质网应激(ERS)并伴随活性氧(ROS)的生成，进而在HCC细胞中触发损伤相关分子模式(DAMP)的释放。相比Cisplatin，ROS-ERS inducer 1 表现出更高的抗癌效能。
T41155	MS 154
	MS 154 is a potent and selective cereblon-recruiting Degrader (PROTAC®) of mutant epidermal growth factor receptor (EGFR), comprising a cereblon-binding moiety joined by a linker to gefitinib(Iressa). MS 154 decreases EGFR protein levels, inhibits downstream signaling in and inhibits proliferation of mutant EGFR-bearing lung cancer cells (DC50values are 11 and 25 nM in HCC-827 and H3255 cells, respectively; Dmax> 95% at 50 nM), but not in WT-EGFR-bearing ovarian and lung cancer cells lines. Bioa...
T79271	FGFR4-IN-14	FGFR	Angiogenesis; Tyrosine Kinase/Adaptors
	FGFR4-IN-14（Compound 27i）是一种高效的FGFR4抑制剂，IC50值仅为2.4 nM。该化合物能够抑制包含V550L和N535K突变的细胞增殖，且在huh7、BaF3/ETV6-FGFR4-V550L和BaF3/ETV6-FGFR4-N535K细胞系中的IC50分别达到21 nM、2.5 nM和171 nM。在Huh7异种移植模型中，FGFR4-IN-14展现出了明显的抗肿瘤效果，适用于肝细胞癌（HCC）的相关研究。
T69395	Nicotinamide-d4
	Nicotinamide-d4 is intended for use as an internal standard for the quantification of nicotinamide by GC- or LC-MS. Nicotinamide is an amide form of niacin, which is also known as vitamin B3, that can be biosynthesized in vivo or obtained through the diet. It is a precursor in the synthesis of the metabolic cofactor NAD+ and an inhibitor of sirtuin 1 (SIRT1; IC50 = <50 µM). Nicotinamide (10 µM) increases the activity of serine palmitoyltransferase (SPT) and the biosynthesis of ceramide, glucosyl...
T62803	STAT3-IN-12
	STAT3-IN-12 是一种 STAT3 的有效信号抑制剂，对 IL-6 诱导的 JAK/STAT3 信号通路的激活具有抑制作用。STAT3-IN-12 对癌细胞生长、迁移具有抑制作用，可阻滞细胞周期并诱导细胞凋亡。STAT3-IN-12 能够用于癌症的相关研究（如肝细胞癌 (HCC) 、食管癌）。
T75134	MC-GGFG-AM-(10Me-11F-Camptothecin)
	MC-GGFG-AM-(10Me-11F-Camptothecin) 是ZW251合成的Linker-Payload偶联物。ZW251是靶向人GPC3的抗体-活性分子偶联物(ADC)，包括人源化IgG1抗体、喜树碱(camptothecin)类的扑异构酶1抑制剂ZD06519及连接子（马来酰亚胺锚定和甘酰甘酰苯丙酰甘氨酸(GGFG)-氨基甲基(AM)可切割连接体）。该药物对人和食蟹猴GPC3具高亲和力，在表达GPC3的HCC细胞系中快速内化并可对GPC3阴性癌细胞进行旁观者介导杀伤。
T35573	Adenosine 5’-methylenediphosphate (hydrate)
	Adenosine 5’-methylenediphosphate is an inhibitor of ecto-5’-nucleotidase, also known as CD73, with a Kivalue of 37 nM.1It inhibits cAMP accumulation induced by adenosine 5’-monophosphate , adenosine 5’-diphosphate , or adenosine 5’-triphosphate but not adenosine in VA-13 human fibroblasts when used at a concentration of 100 μM. Adenosine 5’-methylenediphosphate reduces proliferation of U138MG glioma cells, as well as inhibits the invasion and migration of MHCC97H hepatocellular carcinoma (HCC) ...

化合物

Cat.No: T9945

Synonym: 3-methyl-6-(naphthalen-1-yl)pyrimidine-2,4(1H,3H)-dione

Target: STAT

Amantadine hydrochloride

Cat.No: T1406

Synonym: 盐酸金刚烷胺,1-adamantanamine HCl,1-Adamantanamine hydrochloride,Symmetrel,CI-719,Amantadine HCl,1-Adamantylamine hydrochloride

Target: Dopamine Receptor, Influenza Virus

Anticancer agent 73

Cat.No: T60420

Target: DNA/RNA Synthesis

Cat.No: T60604

Target: Apoptosis, Autophagy

Cat.No: T64529

Synonym: MDL 800,MDL800

Target: Sirtuin

Cat.No: T3226

Synonym: ABT-450,Veruprevir,帕利瑞韦

Target: HCV Protease

Cat.No: T15234

Synonym: IRC 110160,ENMD-119,ENMD 1198

Target: HIF, STAT

Autophagy-IN-C1

Cat.No: T38977

Synonym: Autophagy-IN-C1

Cat.No: T68875

Cat.No: T70988

KRAS G12C inhibitor 43

Cat.No: T64085

Cat.No: T62704

Tubulin polymerization-IN-45

Cat.No: T79341

ROS-ERS inducer 1

Cat.No: T74225

Cat.No: T41155

Cat.No: T79271

Target: FGFR

Nicotinamide-d4

Cat.No: T69395

Cat.No: T62803

MC-GGFG-AM-(10Me-11F-Camptothecin)

Cat.No: T75134

Adenosine 5’-methylenediphosphate (hydrate)

Cat.No: T35573

Cat. No.	Product Name	Target	Signaling Pathways
T7060	Amantadine 1-Aminoadamantane,1-金刚烷胺,金刚烷胺,1-Adamantanamine,1-Adamantylamine	Others	Others
	Amantadine (1-Aminoadamantane) 是抗病毒药物，也是是 NMDA 型谷氨酸受体的弱拮抗剂，能促进高多巴胺的释放，并阻断多巴胺的再摄取。
T13741	Isoviolanthin 异佛莱心苷,异佛来心苷	Others	Others
	Isoviolanthin 是一种黄酮类苷类化合物，提取自铁皮石斛叶中。它能减少 TGF-β1 处理的 HCC 细胞的迁移和入侵能力，对正常细胞没有毒性影响，对转移性肝癌晚期具有潜在的研究价值。
T4A2399	Cinobufotalin 华蟾毒它灵,华蟾素	IL Receptor; Akt; MRP; P-gp	Cytoskeletal Signaling; Immunology/Inflammation; Membrane transporter/Ion channel; Neuroscience; PI3K/Akt/mTOR signaling
	Cinobufotalin 是一种从蟾蜍的皮肤分泌物中提取的强心类固醇或丁二烯内酯。它已被用作强心药，利尿药和止血药，也是潜在的抗肺癌药物。
T5A2455	Arenobufagin 沙蟾毒精,沙蟾毒经	Others	Others
	Arenobufagin 是一种蟾蜍甾烯，从蟾蜍毒液中提取得到，具有抗癌活性。
T2789	Scutellarin 黄岑素,野黄芩苷,Breviscapin,Breviscapinun,Breviscapine,Scutellarein-7-glucuronide	Akt; HIV Protease; STAT	Cytoskeletal Signaling; JAK/STAT signaling; Microbiology/Virology; PI3K/Akt/mTOR signaling; Proteases/Proteasome; Stem Cells
	Scutellarin (Scutellarein-7-glucuronide) 是从黄芩中分离的黄酮，可抑制破骨细胞中 RANKL 介导的 MAPK 和 NF-κB 信号通路，并下调 HCC 细胞中的 STAT3/Girdin/Akt 信号通路。
T5S0761	Nitidine chloride	Apoptosis; ERK; FAK; p38 MAPK; NF-κB; Topoisomerase; STAT; Parasite	Angiogenesis; Apoptosis; Cytoskeletal Signaling; DNA Damage/DNA Repair; JAK/STAT signaling; MAPK; Microbiology/Virology; NF-κB; Stem Cells; Tyrosine Kinase/Adaptors
	Nitidine chloride 是从Zanthoxylum nitidum (Roxb) DC 中分离得到的，具有抗疟疾活性。它通过多个靶点通路，起抗癌作用，抑制STAT3、DNA 拓扑异构酶1和2A、ERK 和c-Src/FAK 相关信号通路。它通过MAPK 和NF-kB 途径抑制Lps 诱导的炎性细胞因子的产生。
T3391	Corosolic acid Corsolic acid,2α-Hydroxyursolic acid,科罗索酸,Glucosol,Colosolic acid,Colosic acid	FAK; Autophagy	Angiogenesis; Autophagy; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors
	Corosolic acid (Colosic acid) 是从大花紫薇中提取的一种天然产物，具有抗肿瘤活性。
T3403	Glabridin 光甘草定,Q-100692,KB-289522,LS-176045	Reactive Oxygen Species; Tyrosinase; GABA Receptor; Antibacterial; PPAR	DNA Damage/DNA Repair; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Neuroscience; NF-κB; Proteases/Proteasome
	Glabridin (KB-289522) 能够结合并激活PPARγ，EC50值为 6115 nM，是一种从Glycyrrhiza glabra 中分到的异黄烷类天然产物。它具有抗炎、抗菌、抗肾炎、抗氧化、抗肿瘤、抗糖尿病、抗骨质疏松、保护神经、保护心血管、清除自由基等作用。

天然产物

Cat.No: T7060

Synonym: 1-Aminoadamantane,1-金刚烷胺,金刚烷胺,1-Adamantanamine,1-Adamantylamine

Target: Others

Cat.No: T13741

Synonym: 异佛莱心苷,异佛来心苷

Target: Others

Cat.No: T4A2399

Synonym: 华蟾毒它灵,华蟾素

Target: IL Receptor, Akt, MRP, P-gp

Cat.No: T5A2455

Synonym: 沙蟾毒精,沙蟾毒经

Target: Others

Cat.No: T2789

Synonym: 黄岑素,野黄芩苷,Breviscapin,Breviscapinun,Breviscapine,Scutellarein-7-glucuronide

Target: Akt, HIV Protease, STAT

Nitidine chloride

Cat.No: T5S0761

Target: Apoptosis, ERK, FAK, p38 MAPK, NF-κB, Topoisomerase, STAT, Parasite

Cat.No: T3391

Synonym: Corsolic acid,2α-Hydroxyursolic acid,科罗索酸,Glucosol,Colosolic acid,Colosic acid

Target: FAK, Autophagy

Cat.No: T3403

Synonym: 光甘草定,Q-100692,KB-289522,LS-176045

Target: Reactive Oxygen Species, Tyrosinase, GABA Receptor, Antibacterial, PPAR

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