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10

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T1643	Penciclovir 喷昔洛韦,BRL 39123,VSA 671	HCV Protease; Antifection; HSV	Microbiology/Virology; Proteases/Proteasome
	Penciclovir (BRL 39123) 是一种疱疹病毒核苷类似物 DNA 聚合酶抑制剂。它作用于HSV1 和 2，IC50分别为 0.04-1.8 μg/mL 和 0.06-4.4 μg/mL。
T8669	3,3',4,4'-Benzophenonetetracarboxylic dianhydride	Others	Others
	3,3',4,4'-Benzophenonetetracarboxylic dianhydride 是一种化合物，用于生产聚酰亚胺薄膜和粘合剂的聚酰亚胺前体。它是一种无毒材料，对人体健康没有已知的不良影响。
T67791	BMS-903452	GPR	Endocrinology/Hormones; GPCR/G Protein
	BMS-903452是一种有效的、具有选择性的 GPR119激动剂，EC50为14 nM。BMS-903452可用于治疗急性和慢性啮齿动物糖尿病。GPR119主要在胰腺 b 细胞和胃肠道肠内分泌细胞中表达，对9种不同的细胞色素 P450酶没有显著的抑制作用(IC50 > 40 μM)，不激活 PXR (EC50>50 μM)，并且对肝脏(HEPG2)细胞系没有毒性。
T12009	Telomerase-IN-1	Telomerase	DNA Damage/DNA Repair
	Telomease-IN-1是一种端粒酶抑制剂（IC50：0.19μM）。Telomease-IN-1通过ER 过度反应（EOR）的内质网应激（ERS）激活hTERT 的表达，然后诱导ERS，导致细胞凋亡。Telomease-IN-1通过表达下游信号分子包括CHOP（CAAT /增强子结合蛋白同源蛋白））和线粒体凋亡途径，导致细胞增殖受到抑制。Telomease-IN-1对端粒酶具有较高的抑制活性，对SMMC-7721细胞具有较高的抗增殖能力，对人正常肝细胞无明显毒性作用。Telomease-IN-1 在异种移植肿瘤模型表现出抗肿瘤活性。
T28815	SM21 perchlorate SM21,SM 21,SM-21
	SM21 is a highly potent antifungal agent (MIC = 0.2-1.6 µg/ml) with no toxic to various human cell lines or bacterial species in vitro and was active against Candida isolates that are resistant to existing antifungal agents.
T78693	Anticancer agent 108
	Anticanceragent 108 (Compound 3.10) 为一种有效P-gp抑制剂，展现抗肿瘤活性，对正常细胞及假正常细胞毒性低，且在С57BL/6小鼠中未发现急性毒性。
T38152	Gilvocarcin M
	Gilvocarcin M is an antibiotic originally isolated from S. gilvotanareus. It is active against S. aureus when used at a concentration of 32 μg/ml. Gilvocarcin M inhibits growth of KB cells (IC50 = 0.52 μg/ml) but has no effect on survival in a P388 mouse model of leukemia when used at doses ranging from 25 to 400 mg/kg. Gilvocarcin M intercalates into bacteriophage PM2 DNA. It is toxic to rats with an intravenous LD50 value of 450 mg/kg.
T68502	Dibrospidium Free Base
	Dibrospidium Free Base is a dispirotripiperazine derivative and alkylating agent with potential antineoplastic and anti-inflammatory activities. The duration of DNA synthesis inhibition in tumor cells was found to correlate with spirobromine antitumor activity. Spirobromin is superior to prospidin by the power of the anti-inflammatory effect. Spyrobromin can diminish the latent period of the development of tumours in the experimental rats at intraperitoneal administration. At intragastric admini...
T66029	3,4-Dehydro-L-proline
	The leguminous shrub,Leucaena leucocephala(Leucaena) is wide‐spread in tropical and subtropical agricultural systems and provides a ready source of protein for livestock. However, the presence of mimosine, a non‐protein, amino acid comprising about 12% of the dry matter in growing tips ofLeucaena, is toxic to animals. Mimosine is degraded rapidly in the rumen to produce 3,4‐dihydroxypyridine (3,4‐DHP) and 2,3‐dihydroxypyridine (2,3‐DHP), both of which remain toxic to animals[1]. 3,4-DHP, as a de...
T35904	O-11
	O-11 is an analog of the fully saturated, 14-carbon fatty acid myristic acid, in which the methylene group at position 11 is replaced with oxygen. It is highly effective and selective at killingTrypanosoma brucei, the protozoan parasite responsible for African sleeping sickness, exhibiting an LD50of less than 1 μM in a cell culture assay.1,2The toxic effects of O-11 appear to be caused by its ability to inhibit the incorporation of a single myristate into the GPI anchor of the variant surface gl...

化合物

Cat.No: T1643

Synonym: 喷昔洛韦,BRL 39123,VSA 671

Target: HCV Protease, Antifection, HSV

3,3',4,4'-Benzophenonetetracarboxylic dianhydride

Cat.No: T8669

Target: Others

Cat.No: T67791

Target: GPR

Telomerase-IN-1

Cat.No: T12009

Target: Telomerase

SM21 perchlorate

Cat.No: T28815

Synonym: SM21,SM 21,SM-21

Anticancer agent 108

Cat.No: T78693

Cat.No: T38152

Dibrospidium Free Base

Cat.No: T68502

3,4-Dehydro-L-proline

Cat.No: T66029

Cat.No: T35904

Cat. No.	Product Name	Target	Signaling Pathways
T3779	Crocin II Crocin 2,西红花苷II,Crocetin gentiobiosylglucosyl ester,藏红花,Tricrocin,Crocin B	Caspase; COX; NO Synthase	Apoptosis; Immunology/Inflammation; Neuroscience; Proteases/Proteasome
	Crocin II (Crocetin gentiobiosylglucosyl ester) 是从栀子果实中分离出来的一种天然产物，具有抗氧化、抗癌和抗抑郁活性。它抑制 iNOS 和 COX-2的蛋白质和 m-RNA 的表达，还抑制NO 产生，IC50值为 31.1 μM。
T4776	Glycerol Glycerin,甘油	Endogenous Metabolite	Metabolism
	Glycerol 是甘油三酯（即脂肪和油）和磷脂的重要成分。它在食品工业中被广泛用作甜味剂和保湿剂以及药物制剂。
TN4801	Piscidinol A	Others	Others
	Piscidinol A is toxic against the 4T1 and HEp2 cancer cell lines, the IC50 of 8.0 ± 0.03 and 8.4 ± 0.01 uM, respectively. It can inhibit NO production in mouse peritoneal macrophages with inhibitory ratios ranging from 39.8±7.7 to 68.2±4.5%.

天然产物

Cat.No: T3779

Synonym: Crocin 2,西红花苷II,Crocetin gentiobiosylglucosyl ester,藏红花,Tricrocin,Crocin B

Target: Caspase, COX, NO Synthase

Cat.No: T4776

Synonym: Glycerin,甘油

Target: Endogenous Metabolite

Cat.No: TN4801

Target: Others

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