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17

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T13183	Top1 inhibitor 1	Others	Others
	Top1 inhibitor 1 is a potent inhibitor of human topoisomerase I (Top1)(IC50: 29 nM).
T28993	TOP1210 TOP 1210,TOP-1210
	TOP1210, a narrow spectrum kinase inhibitor, potently inhibits P38α, Src, and Syk kinase activities.
T25256	Pitstop1 Clathrin inhibitor 1,Clathrin-inhibitor-1,Clathrin IN 1
	Clathrin-IN-1 is a selective clathrin inhibitor that acts by addressing clathrin function in cell physiology with potential applications as an inhibitor of virus and pathogen entry and as a modulator of cell signaling.
T70346	TOP1362
	TOP1362 is a Narrow Spectrum Kinase Inhibitors Demonstrate Promise for the Treatment of Dry Eye Disease and Other Ocular Inflammatory Disorders. TOP1362 strongly inhibited the kinase targets p38α, Syk, Src, and Lck, blocked the rise in p38α expression in hyperosmolar Chang cells, and potently reduced inflammatory cytokine release in cellular models of innate and adaptive immunities. In the EIU model, TOP1362 dose-dependently attenuated the LPS-induced rise in inflammatory cell infiltration and o...
T60200	IndiMitecan LMP776	Topoisomerase	DNA Damage/DNA Repair
	IndiMitecan (LMP776) 是一种具有抗癌活性的拓扑异构酶 I（Top1）抑制剂。
T3181	SW044248	Topoisomerase	DNA Damage/DNA Repair
	SW044248 是非典型拓扑异构酶 I 抑制剂，对 NSCLC 细胞具有选择性毒性。
T24610	Pegamotecan Prothecan,PEG-camptothecin,PEG-beta-CPT	Topoisomerase	DNA Damage/DNA Repair
	Pegamotecan (PEG-camptothecin)是一种拓扑异构酶I(TOP1)抑制剂，具有抗癌活性，它可用于治疗食管癌、非小细胞肺癌和胰腺癌。
T11872L	LMP744 hydrochloride NSC706744 hydrochloride,MJ-III65 hydrochloride	Topoisomerase	DNA Damage/DNA Repair
	LMP744 hydrochloride (NSC-706744 hydrochloride) 是一种是拓扑异构酶 1 抑制剂，显示出抗肿瘤的活性。
T11249	Exatecan 依喜替康,DX-8951,DX-8951f	Topoisomerase	DNA Damage/DNA Repair
	Exatecan (DX-8951f) 是一种 DNA 拓扑异构酶 I (TOP1) 抑制剂，IC50 值为 2.2 μM (0.975 μg/mL)。Exatecan 具有抗肿瘤活性，可用于癌症研究。
T15578	Indotecan NSC-724998,LMP-400	Topoisomerase	DNA Damage/DNA Repair
	Indotecan (LMP-400) 是一种有效的拓扑异构酶 1 抑制剂，对 P388、HCT116和MCF-7 细胞系的IC50值分别为 300、1200和560 nM。
T9088	Topovale ARC111,ARC 111,ARC-111,Topoval	Topoisomerase	DNA Damage/DNA Repair
	Topovale (ARC111) 是一种有效的拓扑异构酶 I 抑制剂。Topovale 抑制缺氧介导的缺氧诱导因子 1alpha 的积累。 Topovale 对一组癌细胞表现出低 nM 细胞毒性。与 P388 细胞相比，在 CPT 抗性拓扑异构酶 I (TOP1) 缺陷的 P388/CPT45 细胞中，Topovale 细胞毒性和 Topovale 诱导的细胞凋亡减少了 > 100 倍。
T68365	Indimitecan HCl
	Indimitecan HCl is a TOP1 inhibitor chemical scaffold.
T11872	LMP744 NSC706744,MJ-III65	Others	Others
	LMP744 is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity.
T60617	Topoisomerase I inhibitor 2
	Topoisomerase I inhibitor 2 是一种高度选择性的DNA 拓扑异构酶 I(Top1) 抑制剂，可抑制Top1活性并导致 DNA 损伤。Topoisomerase I inhibitor 2 阻断 G2/M 期并诱导细胞凋亡，具有抗肿瘤作用。
T62094	Topoisomerase I inhibitor 6
	Topoisomerase I inhibitor 6 (Compound 3) 是一种 Topoisomerase I 的有效抑制剂，可以捕获 DNA-Top1 裂解复合物，在非癌细胞系中具有较小的细胞毒性。Topoisomerase I inhibitor 6 对癌症疾病表现出潜在的研究价值。
T78747	DiPT-4	Topoisomerase	DNA Damage/DNA Repair
	DiPT-4为一种TOP1/PARP1双重抑制剂，可引发癌细胞大量DNA双链断裂(DSB)、细胞周期阻滞及凋亡。DiPT-4具有研究癌症耐药性克服潜力。
T28648	S39625 S-39625,S 39625
	S39625, an E-ring camptothecin keto analogue, is a stable, potent, and selective topoisomerase I inhibitor without being substrates of drug efflux transporters. Nanomolar concentrations of S39625 induces intense and persistent histone gamma-H2AX. The chem

化合物

Top1 inhibitor 1

Cat.No: T13183

Target: Others

Cat.No: T28993

Synonym: TOP 1210,TOP-1210

Cat.No: T25256

Synonym: Clathrin inhibitor 1,Clathrin-inhibitor-1,Clathrin IN 1

Cat.No: T70346

Cat.No: T60200

Synonym: LMP776

Target: Topoisomerase

Cat.No: T3181

Target: Topoisomerase

Cat.No: T24610

Synonym: Prothecan,PEG-camptothecin,PEG-beta-CPT

Target: Topoisomerase

LMP744 hydrochloride

Cat.No: T11872L

Synonym: NSC706744 hydrochloride,MJ-III65 hydrochloride

Target: Topoisomerase

Cat.No: T11249

Synonym: 依喜替康,DX-8951,DX-8951f

Target: Topoisomerase

Cat.No: T15578

Synonym: NSC-724998,LMP-400

Target: Topoisomerase

Cat.No: T9088

Synonym: ARC111,ARC 111,ARC-111,Topoval

Target: Topoisomerase

Indimitecan HCl

Cat.No: T68365

Cat.No: T11872

Synonym: NSC706744,MJ-III65

Target: Others

Topoisomerase I inhibitor 2

Cat.No: T60617

Topoisomerase I inhibitor 6

Cat.No: T62094

Cat.No: T78747

Target: Topoisomerase

Cat.No: T28648

Synonym: S-39625,S 39625

Cat. No.	Product Name	Target	Signaling Pathways
T1123	Camptothecin NSC-100880,Campathecin,喜树碱,(S)-(+)-Camptothecin,CPT	Apoptosis; Influenza Virus; Topoisomerase; Antibiotic; Antifungal	Apoptosis; DNA Damage/DNA Repair; Microbiology/Virology
	Camptothecin (CPT) 属于生物碱类天然产物，是一种 DNA 拓扑异构酶 I (Topo I) 的抑制剂 (IC50=679 nM)，具有特异性。Camptothecin 具有抗肿瘤活性，可以诱导细胞凋亡。
TN4173	Guajadial C	Topoisomerase	DNA Damage/DNA Repair
	Guajadial C acts as a Top1 catalytic inhibitor and can delay Top1 poison-mediated DNA damage. It shows cytotoxicity against five human cancer cell lines.
TN5348	Guajadial F
	Guajadial F acts as a Top1 catalytic inhibitor and can delay Top1 poison-mediated DNA damage. Guajadial F shows cytotoxicity against five human cancer cell lines.
TN4172	Guajadial B	Topoisomerase	DNA Damage/DNA Repair
	Guajadial B acts as a Top1 catalytic inhibitor and delays Top1 poison-mediated DNA damage. Guajadial B shows cytotoxicities against five human cancer cell lines, it is the most effective having an IC50 value of 150 nM toward A549 cells.
T75424	(±)-Evodiamine
	(±)-Evodiamine，一种天然生物碱，作为Top1的抑制剂，展现了抗炎、抗肥胖及抗肿瘤特性。(±)-Evodiamine能够通过诱导细胞凋亡来抑制多种肿瘤细胞的增殖。

天然产物

Cat.No: T1123

Synonym: NSC-100880,Campathecin,喜树碱,(S)-(+)-Camptothecin,CPT

Target: Apoptosis, Influenza Virus, Topoisomerase, Antibiotic, Antifungal

Cat.No: TN4173

Target: Topoisomerase

Cat.No: TN5348

Cat.No: TN4172

Target: Topoisomerase

(±)-Evodiamine

Cat.No: T75424

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