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23

抑制剂 & 化合物

8

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T5858	Sertindole Lu 23-174,舍吲哚	Dopamine Receptor; 5-HT Receptor; Adrenergic Receptor; Autophagy	Autophagy; GPCR/G Protein; Neuroscience
	Sertindole (Lu 23-174) 是一种非典型抗精神病药，可与多巴胺 D2 受体和血清素受体亚型 5-HT1D、5-HT2A 和 5-HT2C 结合，Kd 值分别为 2.7、20、0.14 和 6 nM。
T6019	Volasertib BI 6727,伏拉塞替	Apoptosis; PLK	Apoptosis; Cell Cycle/Checkpoint
	Volasertib (BI 6727) 是一种具有口服活性的高效ATP 竞争性Polo 样激酶 1 抑制剂。它抑制 PLK2 和 PLK3，IC50分别为 5 和 56 nM。它是二氢蝶呤酮衍生物，有抗肿瘤活性，可诱导有丝分裂停滞和细胞凋亡。
T69860	PSB-15160
	PSB-15160是治疗雌激素依赖性肿瘤的化合物，对MCF7(乳腺)、NCI-H460(肺)和SF-268 (NCS)细胞的生长具有抑制作用。
T77762	ROS-generating agent 1	Apoptosis; Ferroptosis; ROS Kinase	Apoptosis; Tyrosine Kinase/Adaptors
	ROS-generating agent 1 具有抗癌活性,通过共价修饰 TrxR 的 Sec-498 残基以生成 ROS。ROS-generating agent 1 降低细胞内 TrxR 蛋白水平，促进 NCI-H460 细胞中 ROS 依赖的性细胞凋亡 (apoptosis) 和铁死亡 (ferroptosis)。
T62867	Microtubule inhibitor 3
	化合物17o（IC50: 14.0 nM，NCI-H460）和17p（IC50: 2.9 nM，NCI-H460）与呋喃基团在纳摩尔水平上对各种人类癌细胞系显示出有效的细胞毒性作用。
T63668	Anticancer agent 16
	Anticancer agent 16 对 HCT-116 细胞系 (IC50: 8.55 μM)、NCI-H460 细胞系 (IC50: 5.41 μM) 和 SKOV3 细胞系 (IC50: 6.4 μM)表现出良好的细胞毒效果。
T62639	Microtubule inhibitor 7
	化合物17o（IC50= 14.0 nM，NCI-H460）和 17p（IC50= 2.9 nM，NCI-H460）与呋喃基团对各种人类癌症细胞系显示出有效的纳摩尔水平的细胞毒活性。
T74340	DNA crosslinker 4 dihydrochloride
	DNA crosslinker 4 (dihydrochloride) 作为高效的DNA小沟结合剂，对NCI-H460、A2780和MCF-7癌细胞表现出显著抑制活性，适用于抗癌研究。
T37540	Amycolatopsin B
	Amycolatopsin B is a bacterial metabolite originally isolated fromAmycolatopsisthat has anticancer activity.1It is cytotoxic to NCI H460 lung and SW620 colon cancer cells (IC50s = 0.28 and 0.14 μM, respectively). 1.Khalil, Z.G., Salim, A.A., Vuong, D., et al.Amycolatopsins A-C: Antimycobacterial glycosylated polyketide macrolides from the Australian soil Amycolatopsis sp. MST-108494J. Antibiot. (Tokyo)70(12)1097-1103(2017)
T74338	DNA crosslinker 2 dihydrochloride
	DNA crosslinker 2 (dihydrochloride)为一种高效DNA小沟结合剂，其结合亲和力(ΔTm)达1.2°C。该化合物对NCI-H460、A2780及MCF-7癌细胞展示出抑制活性，适用于抗癌研究。
T68061	Elinafide
	Elinafide 是一种双萘酰亚胺细胞毒性剂，是 DNA 靶向抗癌剂，在体内体外实验中显示出抗肿瘤活性。
T61765	Microtubule inhibitor 5
	Microtubule inhibitor 5 (compound 17f) is a highly potent cytotoxic agent that inhibits microtubule function. It exhibits a substantial cytotoxic effect on NCI-H460 cells, with an IC50 value of 154.5 nM. Moreover, this compound demonstrates excellent cell permeability [1].
T40212	ATR-IN-4
	ATR-IN-4, a potent inhibitor of ATR (Ataxia telangiectasia mutated gene Rad 3-associated kinase), restricts the growth of DU145 prostate cancer cells and NCI-H460 lung cancer cells, with IC 50 values of 130.9 nM and 41.33 nM, respectively.
T36449	(S)-α-Methylbenzyl Ricinoleamide
	(S)-α-Methylbenzyl ricinoleamide is a fatty acid amide derived from ricinoleic acid and methyl benzylamine. It demonstrates potent growth inhibition of glioma (U251), breast (MCF-7), ovarian (NCI-ADR/RES and OVCAR-3), kidney (786-0), non-small cell lung (NCI-H460), and prostate (PC-3) cancer cells with a mean GI50 value of 6.9 μM.
T37541	Amycolatopsin C
	Amycolatopsin C is a polyketide macrolide originally isolated fromAmycolatopsisthat has antimycobacterial and anticancer activities.1It is active againstM. bovisandM. tuberculosis(IC50s = 2.7 and 5.7 μM, respectively) but notB. subtilis,S. aureus,E. coli, orP. aeruginosa(IC50s = >30 μM for all). Amycolatopsin C is cytotoxic to SW620 colorectal and NCI H460 lung cancer cells (IC50s = 10 and 5.9 μM, respectively). 1.Khalil, Z.G., Salim, A.A., Vuong, D., et al.Amycolatopsins A-C: Antimycobacterial ...
T62448	Microtubule inhibitor 6
	Microtubule inhibitor 6 (compound 17o) 是一种有效的微管抑制剂。Microtubule inhibitor 6 对 NCI-H460 细胞、BxPC-3 细胞、HT-29 细胞表现出细胞毒性，他们的 IC50 值分别为 14.0、6.6、7.0 nM。Microtubule inhibitor 6 能够有效抑制微管聚合。
T79451	WES-1	Carbonic Anhydrase	Metabolism
	WES-1（Compound 8g）是一种针对碳酸酐酶IX的抑制剂，其抑制常数（Ki）为55.9 μM。该化合物对包括白血病细胞系（K-562、MOLT-4）、非小细胞肺癌（NCI-H460）、结肠癌（HCT 116、HCT-15）以及黑色素瘤（LOX IMVI）在内的多种癌细胞表现出抗增殖效果。
T78780	Anticancer agent 139
	Anticanceragent 139（Compound 6h）展现了针对多种癌细胞株的抗癌效能。该化合物能够与Tubulin的Lys352残基发生π-阳离子相互作用。在对SNB-19、OVCAR-8和NCI-H460细胞株的测试中，Anticanceragent 139展现出较高的生长抑制率（PGI），数值分别为86.61、85.26和75.99。同时，该化合物对于HOP-62、SNB-75、ACHN、NCI/ADR-RES、786-O、A549/ATCC、HCT-116以及MDA-MB-231细胞株亦表现出中等的生长抑制作用，其PGI值分别为67.55、65.46、59.09、59.02、57.88、56.88、56.53和56.4、51.88。
T37539	Amycolatopsin A
	Amycolatopsin A is a macrolide polyketide originally isolated fromAmycolatopsisthat has antimycobacterial and anticancer activities.1It is active againstM. bovisandM. tuberculosis(IC50s = 0.4 and 4.4 μM, respectively) but notB. subtilis,S. aureus,E. coli, orP. aeruginosa(IC50s = >30 μM for all). Amycolatopsin A is cytotoxic to SW620 colorectal and NCI H460 lung cancer cells (IC50s = 0.08 and 1.2 μM, respectively). 1.Khalil, Z.G., Salim, A.A., Vuong, D., et al.Amycolatopsins A-C: Antimycobacteria...
T83865	HP661
	HP661是一种针对线粒体复合物I（也称为NADH脱氢酶）的抑制剂，对复合物I具有选择性，以1 µM的浓度抑制其77.6%，而对复合物III抑制率为28.1%，对复合物II和IV则无抑制作用。HP661特异性降低具有高水平氧化磷酸化作用的人类肺癌细胞H460、NCI H441及对trametinib耐药的A549细胞的生存能力（IC50分别为10.6、29.7和15.1 nM），相较于氧化磷酸化水平低的NCI H358人类肺癌细胞（IC50 >10,000 nM）以及非癌性人类胰腺正常上皮细胞（HPNE）和MRC-5人类胎肺成纤维细胞（两者的IC50均>10,000 nM）。当以每天两次，每次30 mg/kg的剂量给药时，HP661在H460小鼠异种移植模型中减少肿瘤体积，并对trametinib引导的肿瘤生长减少产生加成效应。
T37006	Previridicatumtoxin
	Previridicatumtoxin is a fungal metabolite that has been found inP. aethiopicumand has diverse biological activities.1,2It is an intermediate in the biosynthesis of the mycotoxin viridicatumtoxin . Previridicatumtoxin is active against methicillin-resistantS. aureus(MRSA) and vancomycin-resistantE. faecalis(IC50s = 4.4 and 4.8 μM, respectively), as well asC. albicansandS. cerevisiae(MIC = 32 μg/ml for both).2,1It is cytotoxic to NCI H460, KB-3-1, and SW620 cancer cells (IC50s = 5.3, 4.1, and 6 μ...
T62642	Microtubule inhibitor 4
	Microtubule inhibitor 4 (compound 2) 是一种有效的 microtubule 抑制剂。Microtubule inhibitor 4 对 NCI-H460 (IC50s: 4.0 nM)、BxPC-3 (IC50s: 3.2 nM)、HT-29 (IC50s: 2.1 nM) 细胞具有细胞毒性。Microtubule inhibitor 4 能够抑制微管蛋白聚合。
T13226	Tubulin inhibitor 8	Microtubule Associated	Cytoskeletal Signaling
	Tubulin inhibitor 8是管蛋白和多种癌症细胞系的抑制剂，对管蛋白聚合和K562细胞生长具有抑制作用，IC50分别为0.73μM 和14nM。

化合物

Cat.No: T5858

Synonym: Lu 23-174,舍吲哚

Target: Dopamine Receptor, 5-HT Receptor, Adrenergic Receptor, Autophagy

Cat.No: T6019

Synonym: BI 6727,伏拉塞替

Target: Apoptosis, PLK

Cat.No: T69860

ROS-generating agent 1

Cat.No: T77762

Target: Apoptosis, Ferroptosis, ROS Kinase

Microtubule inhibitor 3

Cat.No: T62867

Anticancer agent 16

Cat.No: T63668

Microtubule inhibitor 7

Cat.No: T62639

DNA crosslinker 4 dihydrochloride

Cat.No: T74340

Amycolatopsin B

Cat.No: T37540

DNA crosslinker 2 dihydrochloride

Cat.No: T74338

Cat.No: T68061

Microtubule inhibitor 5

Cat.No: T61765

Cat.No: T40212

(S)-α-Methylbenzyl Ricinoleamide

Cat.No: T36449

Amycolatopsin C

Cat.No: T37541

Microtubule inhibitor 6

Cat.No: T62448

Cat.No: T79451

Target: Carbonic Anhydrase

Anticancer agent 139

Cat.No: T78780

Amycolatopsin A

Cat.No: T37539

Cat.No: T83865

Previridicatumtoxin

Cat.No: T37006

Microtubule inhibitor 4

Cat.No: T62642

Tubulin inhibitor 8

Cat.No: T13226

Target: Microtubule Associated

Cat. No.	Product Name	Target	Signaling Pathways
TN4355	Jolkinol A	Others	Others
	Jolkinol A can inhibit both MCF-7 (breast adenocarcinoma), NCI-H460 (non-small cell lung cancer) cell lines, with GI50 values ranging between 40.9 microM and 95.3 microM.
T75524	Mutabilol
	Mutabilol (compound 1) 是一种有效的 p-糖蛋白 (P-gp) 调节剂。Mutabilol 是一种可以从Plectranthus mutabilis 叶中分离得到的天然产物。Mutabilol 增加 NCI-H460/R 细胞中P-gp 的表达。
TN4387	Khellactone	Antifection	Microbiology/Virology
	Khellactone shows antitumor activity,it can suppress the growth of NCI-H460 tumor cells. (+)-4'-cis-Khellactone and (+)-3'-cis-khellactone have antiplasmodial activities, they show notable inhibitory activity against -sensitive strains of with IC(50) values from 1.5 and 2.4 microM.
T72803	Norartocarpetin
	Norartocarpetin 是一种酪氨酸酶抑制剂。Norartocarpetin 具有较强的酪氨酸酶抑制活性，其抑制活性 IC50值为 0.47 μM。Norartocarpetin 作为一种抗褐变剂可用于食品体系的研究。Norartocarpetin 对肺癌细胞 (NCI-H460) 也具有显著的抗癌活性，其 IC50值为 22 μM。Norartocarpetin 的抗增殖作用是通过靶向 Ras/Raf/MAPK 信号通路、线粒体介导的细胞凋亡、S 期细胞周期阻滞和抑制细胞迁移和侵袭实现的。
TN5930	Ocotillone
	Ocotillone has potent antibacterial activity against Gram-negative bacteria, P. aeruginosa and S. typhimurium, that are without hemolytic activity, whereas it has weak antimicrobial activity against Gram-positive bacteria and fungi. Ocotillone shows only
T81201	Sartorypyrone B
	Sartorypyrone B为Chevalone C的2β-乙酰氧基衍生物，由海绵源真菌Neosartorya tsunodae(KUFC 9213)的培养物中乙酸乙酯提取得到。该化合物对MCF-7、NCI-H460和A375-C5细胞系展示出较强的生长抑制活性，GI50s值分别为17.8、20.5和25.0 μM，显示其在乳腺癌、非小细胞肺癌和黑色素瘤研究中的应用潜力。
T35754	Aszonapyrone A
	Aszonapyrone A is a meroditerpene fungal metabolite that has been found in Neosartorya and has diverse biological activities.1,2,3 It inhibits the growth of MCF-7, NCI H460, and A375-C5 cancer cells (GI50s = 13.6, 11.6, and 10.2 μM, respectively).1 Aszonapyrone A is active against multidrug-resistant isolates of S. aureus, E. faecalis, and E. faecium (MICs = 8, 16, and 16 μg/ml, respectively) and inhibits S. aureus biofilm formation.2 It is also active against P. falciparum in vitro (IC50 = 1.34...
T36489	Malformin A
	Malformin A is a cyclopentapeptide fungal metabolite that has been found in A. niger and has diverse biological activities. It is a plant growth regulator that induces malformations in plant structure. Malformin A inhibits replication of tobacco mosaic virus (TMV) in local lesion and leaf-disc assays (IC50s = 19.7 and 45.4 μg/ml, respectively). It is cytotoxic to NCI-H460, MIA PaCa-2, MCF-7, SF-268, and WI-38 cancer cells (IC50s = 70, 50, 100, 70, and 100 nM, respectively), inhibits proliferati...

天然产物

Cat.No: TN4355

Target: Others

Cat.No: T75524

Cat.No: TN4387

Target: Antifection

Norartocarpetin

Cat.No: T72803

Cat.No: TN5930

Sartorypyrone B

Cat.No: T81201

Cat.No: T35754

Cat.No: T36489

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