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13

抑制剂 & 化合物

13

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T6738	Z-FA-FMK	SARS-CoV; Cysteine Protease	Microbiology/Virology; Proteases/Proteasome
	Z-FA-FMK 是一种广谱的卤代甲基酮抑制剂，可抑制冠状病毒蛋白酶3CL，Ki 为 25.7 μM。它可以不可逆地抑制半胱氨酸蛋白酶，也可以抑制效应半胱天冬酶。
T1772	MDK83190 Apoptosis Activator 2	Apoptosis; Caspase	Apoptosis; Proteases/Proteasome
	MDK83190 (Apoptosis Activator 2) 是一种细胞凋亡激活剂，可诱导 caspase-3 激活、Apaf-1 寡聚化、PARP 切割和 DNA 片段化。
T9743	FEN1-IN-SC13	Others	Others
	FEN1-IN-SC13 是有效的DNA 片段化核酸内切酶 1 抑制剂。
T22812	GRI977143 GRI 977143	LPA Receptor	GPCR/G Protein
	GRI977143 是 LPA2 的选择性非脂质激动剂 (EC50 = 3.3 μM)。 GRI977143 抑制半胱天冬酶 3、7、8 和 9 的激活，并减少 DNA 片段化。
T68896	Daniquidone NSC 320846,BAY-H 2049	Topoisomerase	DNA Damage/DNA Repair
	Daniquidone (Batracylin) 是一种有效的 DNA 拓扑异构酶 I 和 DNA 拓扑异构酶 II 双重抑制剂，具有细胞毒性和抗增殖活性，可诱导 DNA 断裂，可用于研究肿瘤、免疫系统疾病和淋巴系统疾病。
T25856	NC182 NC 182,NC-182
	NC182 is a topo II inhibitor that shows selective and potent topo II inhibition on the induction of topo II-dependent DNA fragmentation.
T69896	Sabarubicin MEN 10755
	Sabarubicin 是一种阿霉素双糖类似物，具有显著的抗肿瘤活性。Sabarubicin 作为一种拓扑异构酶 II 毒药比阿霉素更有效，并在较低的细胞内浓度下刺激 DNA 片段。
T62555	MMP-2/9-IN-1
	MMP-2/9-IN-1 (Compound 4a) 是一种有效的 MMP-2 (IC50: 56 nM) 和 MMP-9 (IC50: 38 nM) 双重抑制剂。MMP-2/9-IN-1 对肿瘤生长具有抑制作用，明显诱导癌细胞凋亡 (apoptosis)，抑制细胞迁移，并抑制细胞周期进程导致 DNA 片段化。
T36324	C8 L-threo Ceramide (d18:1/8:0) C8 L-threo Ceramide (d18:1/8:0)
	C8 L-threo Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. It is cytotoxic to U937 cells (IC50 = 10 μM) and, like C8 D-threo ceramide , induces nuclear DNA fragmentation 5- to 6-fold more potently than C8 L-erythro ceramide . C8 D-threo Ceramide also enhances V. cholerae cytolysin pore formation in liposome lipid membranes, as measured by calcein release, with a 50% release dose (RD50) value of ~30 μg/ml.
T36322	C8 D-threo Ceramide (d18:1/8:0) C8 D-threo Ceramide (d18:1/8:0)
	C8 D-threo Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. It is cytotoxic to U937 cells (IC50 = 17 μM) and induces nuclear DNA fragmentation 5- to 6-fold more potently than C8 ceramide . C8 D-threo Ceramide is a substrate for E. coli diacylglycerol kinase. It activates ceramide-activated protein kinase (CAPK) in U937 cells. C8 D-threo Ceramide also enhances V. cholerae cytolysin pore formation in liposome lipid membranes, as measured by calcein r...
T36671	C2 Phytoceramide (t18:0/2:0)
	C2 Phytoceramide is a bioactive semisynthetic sphingolipid that inhibits formyl peptide-induced oxidant release (IC50 = 0.38 μM) in suspended polymorphonuclear cells. It increases COX-2 protein levels 15-fold through ERK signaling. It induces death of keratinocytes (20% viability) with an ED50 value of 30 μM, the same concentration at which 35% of cells in a TUNEL assay are apoptotic. C2 Phytoceramide also has antiproliferative effects in CHO cells, with greater than 80% cytotoxicity achieved at...
T69323	Dexamethasone sodium succinate
	Dexamethasone sodium succinate is the acetate salt form of dexamethasone, which is a synthetic glucocorticoid; it combines high anti-inflammatory effects with low mineralocorticoid activity. At high doses (e.g. 40 mg), it reduces the immune response. Dexamethasone acetate (NEOFORDEX®) is indicated in adults for the treatment of symptomatic multiple myeloma in combination with other medicinal products. Dexamethasone has been shown to induce multiple myeloma cell death (apoptosis) via a down-regul...
T36410	9(E),11(E),13(E)-Octadecatrienoic Acid
	9(E),11(E),13(E)-Octadecatrienoic acid (β-ESA) is a conjugated polyunsaturated fatty acid that is found in plant seed oils and in mixtures of conjugated linolenic acids synthesized by the alkaline isomerization of linolenic acid. It reduces growth of Caco-2 colon cancer cells in a dose-dependent and time-dependent manner. In vitro, β-ESA induces DNA fragmentation and upregulation of pro-apoptotic Bax mRNA. β-ESA decreases protein expression of the apoptosis suppression factor Bcl-2 and induces a...

化合物

Cat.No: T6738

Target: SARS-CoV, Cysteine Protease

Cat.No: T1772

Synonym: Apoptosis Activator 2

Target: Apoptosis, Caspase

Cat.No: T9743

Target: Others

Cat.No: T22812

Synonym: GRI 977143

Target: LPA Receptor

Cat.No: T68896

Synonym: NSC 320846,BAY-H 2049

Target: Topoisomerase

Cat.No: T25856

Synonym: NC 182,NC-182

Cat.No: T69896

Synonym: MEN 10755

Cat.No: T62555

C8 L-threo Ceramide (d18:1/8:0)

Cat.No: T36324

Synonym: C8 L-threo Ceramide (d18:1/8:0)

C8 D-threo Ceramide (d18:1/8:0)

Cat.No: T36322

Synonym: C8 D-threo Ceramide (d18:1/8:0)

C2 Phytoceramide (t18:0/2:0)

Cat.No: T36671

Dexamethasone sodium succinate

Cat.No: T69323

9(E),11(E),13(E)-Octadecatrienoic Acid

Cat.No: T36410

Cat. No.	Product Name	Target	Signaling Pathways
TN3110	5-Geranoxy-7-methoxycoumarin	Anti-infection; Antibacterial; Antifungal	Microbiology/Virology
	5-Geranoxy-7-methoxycoumarin 是一种香豆素。它诱导细胞凋亡，具有抗癌、抗真菌和抗菌活性。
T4730	Thymidine-5'-monophosphate disodium salt 胸苷酸二钠,Thymidine 5'-monophosphate disodium salt,TMP DISODIUM SALT	Others; Endogenous Metabolite	Metabolism; Others
	Thymidine-5'-monophosphate disodium salt (TMP DISODIUM SALT) 是内源性代谢产物的一种。
T5S0636	Citric acid 柠檬酸,Citro,Citretten	Apoptosis; Others; Endogenous Metabolite; Antibacterial; Antibiotic	Apoptosis; Metabolism; Microbiology/Virology; Others
	Citric acid (Citro) 是柑橘类水果中发现的弱有机三羧酸。柠檬酸是食品添加剂和天然防腐剂。
TN3049	4-Methoxycinnamyl alcohol	Others	Others
	4-Methoxycinnamyl alcohol 对MCF-7、HeLa 和DU145癌症细胞系显示出毒性，IC50值分别为14.24、7.82和22.10μg/mL。4-methoxycinnamyl alcohol 是从Foeniculum vulgare 中分离出来的。4-Methoxycinnamyl alcohol 没有显示出凋亡作用，却在10μg/mL DNA 碎片研究显示48小时后发生了坏死。
T2220	2-Methoxyestradiol 2-甲氧雌二醇,二甲氧基雌二醇,NSC-659853,2-MeOE2,2-ME2	Apoptosis; Reactive Oxygen Species; Microtubule Associated; Endogenous Metabolite; HIF; Autophagy	Angiogenesis; Apoptosis; Autophagy; Chromatin/Epigenetic; Cytoskeletal Signaling; Immunology/Inflammation; Metabolism; NF-κB
	2-Methoxyestradiol (2-ME2) 是一种口服生物可利用的雌二醇代谢物，具有抗肿瘤活性。它通过减少内皮细胞增殖和诱导内皮细胞凋亡来抑制血管生成，也可破坏微管的稳定。它可诱导半胱天冬酶活化，导致细胞周期停滞在 G2 期、DNA 断裂和细胞凋亡。
TN2496	1,4-Anthraquinone	Others	Others
	1,4-Anthraquinone 是一种抗癌药物，在体外与柔红霉素相同纳摩尔范围内阻断核苷转运、抑制大分子合成、诱导 DNA 片段化并降低 L1210 白血病细胞的生长和活力。它被提议为一种用于高效液相色谱 (HPLC) 测定药物制剂中 N-乙酰半胱氨酸 (NAC) 和卡托普利 (CAP) 的新型柱前试剂。
T9113	Myristicin Myristicine,肉豆蔻醚	IL Receptor; Anti-infection; BCL; P450; PARP; 5-HT Receptor; Caspase; GABA Receptor; NO Synthase	Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair; GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Neuroscience; Proteases/Proteasome
	Myristicin (Myristicine) 是一种在香料和伞形植物中发现的天然产物。肉豆蔻素具有抗胆碱能、抗菌和肝保护作用，还具有抗炎作用，其通过钙途径抑制dsrna 刺激的巨噬细胞中的NO、细胞因子、趋化因子和生长因子。Myristicin 可以诱导细胞凋亡，其特征是改变线粒体膜电位、细胞色素c 释放、Caspase-3激活、parp 切割和DNA 断裂。
T75645	Echitamine chloride
	Echitamine chloride 是存在于 Alstonia scholaris 中的主要单萜吲哚生物碱，具有有效的抗肿瘤活性。Echitamine chloride 会诱导 DNA 片段化和细胞凋亡 (apoptosis)。Echitamine chloride 抑制胰腺脂肪酶 (pancreatic lipase)，IC50为 10.92 µM。
T73068	Mammea A/BA
	Mammea A/BA 对克氏锥虫 (T. cruzi) 显示出有效抗性。通过诱导线粒体功能障碍、产生活性氧 (ROS)、DNA 片段化以及增加酸性液泡数量，Mammea A/BA 触发细胞死亡机制，包括细胞凋亡 (apoptosis)、细胞自噬 (autophagy) 和细胞坏死，对于南美锥虫病的研究具有潜在应用价值。
T35647	4-oxo-27-TBDMS Withaferin A
	4-oxo-27-TBDMS Withaferin A is a derivative of the steroidal lactone withaferin A that has anticancer activity.1 It is cytotoxic to A2780 ovarian cancer cells (IC50 = 17 μM) but not to carboplatin-resistant A2780 (A2780/CP70) cells (IC50 = >100 μM). It is selective for A2780 cells over non-cancerous ARPE19 cells (IC50 = 1,660 μM). 4-oxo-27-TBDMS Withaferin A induces DNA fragmentation in A2780 cells.References1. Perestelo, N.R., Llanos, G.G., Reyes, C.P., et al. Expanding the chemical space of wi...
TN4475	Macrocarpal C	ROS; Antifection	Immunology/Inflammation; Microbiology/Virology
	Macrocarpal C, isolated from the fresh leaves of Eucalyptus globulus Labill. (Lan An) and identified as its major antifungal component by bioassay-guided purification, the antifungal action of macrocarpal C was associated with increases of membrane permea
TN2945	3-Hydroxybakuchiol	ATPase; Caspase	Apoptosis; Membrane transporter/Ion channel; Proteases/Proteasome
	3-Hydroxybakuchiol exerts cytotoxic and anti-proliferative effects on the TA3/Ha mouse mammary adenocarcinoma cell line and induces a decrease in the mitochondrial transmembrane potential, the activation of caspase-3, the opening of the mitochondrial perm
T36954	Nemorosone
	Nemorosone is a polycyclic polyprenylated acylphloroglucinol (PPAP) originally isolated from C. rosea that has antiproliferative properties.1 Nemorosone inhibits growth of NB69, Kelly, SK-N-AS, and LAN-1 neuroblastoma cells (IC50s = 3.1-6.3 μM), including several drug-resistant clones, but not MRC-5 human embryonic fibroblasts (IC50 = >40 μM).2 It increases DNA fragmentation in LAN-1 cells in a dose-dependent manner, and decreases N-Myc protein levels and phosphorylation of ERK1/2 by MEK1/2. Nem...

天然产物

5-Geranoxy-7-methoxycoumarin

Cat.No: TN3110

Target: Anti-infection, Antibacterial, Antifungal

Thymidine-5'-monophosphate disodium salt

Cat.No: T4730

Synonym: 胸苷酸二钠,Thymidine 5'-monophosphate disodium salt,TMP DISODIUM SALT

Target: Others, Endogenous Metabolite

Cat.No: T5S0636

Synonym: 柠檬酸,Citro,Citretten

Target: Apoptosis, Others, Endogenous Metabolite, Antibacterial, Antibiotic

4-Methoxycinnamyl alcohol

Cat.No: TN3049

Target: Others

2-Methoxyestradiol

Cat.No: T2220

Synonym: 2-甲氧雌二醇,二甲氧基雌二醇,NSC-659853,2-MeOE2,2-ME2

Target: Apoptosis, Reactive Oxygen Species, Microtubule Associated, Endogenous Metabolite, HIF, Autophagy

1,4-Anthraquinone

Cat.No: TN2496

Target: Others

Cat.No: T9113

Synonym: Myristicine,肉豆蔻醚

Target: IL Receptor, Anti-infection, BCL, P450, PARP, 5-HT Receptor, Caspase, GABA Receptor, NO Synthase

Echitamine chloride

Cat.No: T75645

Cat.No: T73068

4-oxo-27-TBDMS Withaferin A

Cat.No: T35647

Cat.No: TN4475

Target: ROS, Antifection

3-Hydroxybakuchiol

Cat.No: TN2945

Target: ATPase, Caspase

Cat.No: T36954

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