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26

抑制剂 & 化合物

6

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T8756	KRAS inhibitor-9 DUN09716	Apoptosis; Ras	Apoptosis; GPCR/G Protein; MAPK
	KRAS inhibitor-9 (DUN09716) 是一种 KRAS 抑制剂，阻止 GTP-KRAS 的形成和 KRAS 下游激活。它以中等的结合亲和力与 KRAS G12D、KRAS G12C 和 KRAS Q61H 蛋白结合，选择性抑制具有 KRAS 突变的 NSC-LC 细胞的增殖。它可导致 G2/M 细胞周期停滞并诱导凋亡。
TQ0059	Ilorasertib ABT-348	VEGFR; FLT; c-RET; PDGFR; Aurora Kinase	Angiogenesis; Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Tyrosine Kinase/Adaptors
	Ilorasertib (ABT-348) 是一种 ATP 竞争性多靶点激酶抑制剂，可抑制 Aurora A、Aurora B 和Aurora C，IC50值为120 nM、7 nM 和1 nM。它还抑制 RET 酪氨酸激酶、PDGFRβ 和 Flt1，IC50为7 nM、3 nM 和 32 nM。
T9003	CVT-11127 N-[2-[6-[[(3,4-二氯苯基)甲基]氨基]-2-(4-甲氧基苯基)-3-氧代-3,4-二氢吡啶并[2,3-B]吡嗪-4-基]乙基]乙酰胺	Dehydrogenase	Metabolism
	CVT-11127 是 SCD 抑制剂。它将细胞周期阻滞在 G1/S 期，诱导细胞凋亡。它可用于肺癌的研究。
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)。
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。
T83892	33-BCRP Inhibitor 33-Breast Cancer Resistance Protein Inhibitor
	33-BCRP抑制剂是一种乳腺癌耐药蛋白(BCRP)的抑制剂。它使得对米托蒽醌耐药的H460/MX20肺癌细胞对米托蒽醌诱导的细胞死亡更加敏感，无论是单独使用还是与UV辐射联合使用。33-BCRP抑制剂还能够增强表达P-糖蛋白(P-gp，亦称为多药耐药蛋白MDR)的KB-C2表皮癌细胞对秋水仙碱诱导的细胞死亡的敏感性。当使用5 µM浓度时，它能增加米托蒽醌在H460/MX20细胞中的细胞内积累。
T38382	8Br-HA
	8Br-HA is an inhibitor of fragile histidine triad diadenosine triphosphatase (FHIT; IC50= 0.12 μM).1It inhibits the growth of HCC827 and H460 lung cancer cells (GI50s = 0.87 and 5.9 μM, respectively). 1.Kawaguchi, M., Sekimoto, E., Ohta, Y., et al.Synthesis of fluorescent probes targeting tumor-suppressor protein FHIT and Identification of apoptosis-inducing FHIT inhibitorsJ. Med. Chem.64(13)9567-9576(2021)
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)
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.
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。
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].
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 ...
T61996	Antiproliferative agent-6
	Antiproliferative agent-6 (compound 8a) 是有效的抗肿瘤化合物。Antiproliferative agent-6 具有抗增殖活性，抑制癌细胞系 HCT116、MCF-7、H460 和非肿瘤非整倍体永生角质细胞 HaCaT 的 GI50分别为 0.5 μM、2 μM、0.7 μM 和 3.5 μM。
T83011	Antitumor agent-105
	Antitumor agent-105（Compound 37）是一种对A549、H1299、H460、HCT116、MDA-MB-231细胞线显示出抗肿瘤活性的化合物，其IC50值分别为6.7、8.3、4.3、4.4、6.7μM。
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。
T37758	Unguinol
	Unguinol is a depsidone originally isolated from A. unguis. It is an inhibitor of pyruvate phosphate dikinase (PPDK; IC50 = 42.3 μM). It inhibits the growth of plants utilizing C4, but not C3, carbon fixation. Unguinol also inhibits the growth of the bacteria S. aureus and V. harveyi (GI50s = 8.7 and 69.5 μM, respectively) and H460, MCF-7, and SF-268 cancer cells (GI50s = 28.2, 50.8, and 44.3 μM, respectively).
T63590	c-Met-IN-10
	c-Met-IN-10 是高效的 c-Met 激酶抑制剂 (IC50: 16 nM)。c-Met-IN-10 能够抑制癌细胞 A549、H460 和 HT-29 的活性，通过抑制 HT-29 细胞集落形成，进而诱导 HT-29 和 A549 细胞凋亡 apoptosis，抑制 A549 细胞移动。c-Met-IN-10 能够用于抗癌研究。
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.
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。
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...
T70856	3-Oxobetulin Acetate
	3-Oxobetulin acetate is a derivative of the cholesterol biosynthesis inhibitor betulin. It inhibits the growth of P388 murine lymphocytic leukemia cells (EC50 = 0.12 µg/ml), as well as human MCF-7 breast, SF-268 CNS, H460 lung, and KM20L2 colon cancer cells (GI50s = 8, 10.6, 5.2, and 12.7 µg/ml, respectively), but not BxPC-3 pancreas or DU145 prostate cancer cells (GI50s = >10 µg/ml for both). 3-Oxobetulin acetate inhibits replication of X4 tropic recombinant HIV (NL4.3-Ren) in MT-2 lymphoblasto...
T35438	(5E)-7-Oxozeaenol
	(5E)-7-Oxozeaenol is a resorcylic acid lactone that has been found in the fungus MSX 63935 and has enzyme inhibitory and anticancer activities.1,2 It inhibits TGF-β-activated kinase 1 (TAK-1; IC50 = 1.3 μM).1 (5E)-7-Oxozeaenol inhibits proliferation of MCF-7, H460, SF-268, HT-29, and MDA-MB-435 human cancer cells with IC50 values of 4.9, 1.2, 5.6, 4.4, and 5.5 μM, respectively.2 \|1. Fakhouri, L., El-Elimat, T., Hurst, D.P., et al. Isolation, semisynthesis, covalent docking and transforming growt...
T35675	SW203668 (trifluoroacetate salt)
	SW203668 is an irreversible inhibitor of stearoyl-CoA desaturase (IC50 = 54 nM). It is selectively cytotoxic to H2122, H460, HCC44, and HCC95 cell lines that express cytochrome P450 (CYP) isoform CYP4F11 over eight other cancer cell lines that lack CYP4F11 in vitro (IC50s = 22-116 and >10,000 nM, respectively) and ectopic expression of CYP4F11 in SW203668-insensitive H1155 cells results in sensitization to SW203668. In vivo, SW203668 reduces tumor growth rate without reducing sebocyte production...
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。

化合物

KRAS inhibitor-9

Cat.No: T8756

Synonym: DUN09716

Target: Apoptosis, Ras

Cat.No: TQ0059

Synonym: ABT-348

Target: VEGFR, FLT, c-RET, PDGFR, Aurora Kinase

Cat.No: T9003

Synonym: N-[2-[6-[[(3,4-二氯苯基)甲基]氨基]-2-(4-甲氧基苯基)-3-氧代-3,4-二氢吡啶并[2,3-B]吡嗪-4-基]乙基]乙酰胺

Target: Dehydrogenase

Cat.No: T69860

ROS-generating agent 1

Cat.No: T77762

Target: Apoptosis, Ferroptosis, ROS Kinase

Cat.No: T68061

33-BCRP Inhibitor

Cat.No: T83892

Synonym: 33-Breast Cancer Resistance Protein Inhibitor

Cat.No: T38382

Amycolatopsin B

Cat.No: T37540

Cat.No: T40212

Tubulin inhibitor 8

Cat.No: T13226

Target: Microtubule Associated

Microtubule inhibitor 5

Cat.No: T61765

Amycolatopsin C

Cat.No: T37541

Antiproliferative agent-6

Cat.No: T61996

Antitumor agent-105

Cat.No: T83011

Microtubule inhibitor 6

Cat.No: T62448

Cat.No: T37758

Cat.No: T63590

(S)-α-Methylbenzyl Ricinoleamide

Cat.No: T36449

Cat.No: T83865

Amycolatopsin A

Cat.No: T37539

3-Oxobetulin Acetate

Cat.No: T70856

(5E)-7-Oxozeaenol

Cat.No: T35438

SW203668 (trifluoroacetate salt)

Cat.No: T35675

Previridicatumtoxin

Cat.No: T37006

Microtubule inhibitor 4

Cat.No: T62642

Cat. No.	Product Name	Target	Signaling Pathways
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
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: T75524

Cat.No: TN4387

Target: Antifection

Norartocarpetin

Cat.No: T72803

Cat.No: TN5930

Cat.No: T35754

Cat.No: T36489

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