h460 cells

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。

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。

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。

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。

Merestinib dihydrochloride (LY2801653 dihydrochloride) 是一种可口服的激酶抑制剂，具有抗肿瘤活性，抑制 MET、AXL、RON 和 MKNK1/2，抑制 NTRK 融合携带肿瘤的生长。

Colcemid (NSC-3096) 是一种微管聚合抑制剂,主要靶点是微管蛋白 (Tubulin)，IC50=2.4 μM。Colcemid 可诱导细胞凋亡，可用于肿瘤和胚胎克隆的研究。

Dynole 34-2(Dynamin Inhibitor V, 34-2)是一种强效和非竞争性的的dynamin1和dynamin2 GTPase抑制剂，通过靶向GTPase结构域的变构位点，抑制受体介导的内吞作用和突触囊泡内吞作用。Dynole 34-2在多种细胞系中表现出抗有丝分裂作用，诱导细胞凋亡。

IACS-010759 hydrochloride是一种口服有效和选择性的OXPHOS抑制剂,在依赖 OXPHOS 的脑癌和急性髓性白血病模型中抑制增殖并诱导细胞凋亡，可用于研究复发/难治性 AML 和晚期实体瘤。

Arcyriaflavin A 来源于 Eudistoma sp，对D1-CDK4 、B–CDK1和CaMKII具有抑制作用，IC50值分别为0.14μM、1.13μM和0.025μM，同时对HCT-116和NCI-H460细胞具有抑制作用，IC50值分别为0.85μM和0.59μM。

And1 degrader 1（Compound A15）作为酸性核质DNA结合蛋白1（And1）的特定降解剂，在NSCLC细胞中有效触发And1的降解。在5 μM浓度下，该化合物与Olaparib（1 μM）合用，显著抑制了A549及H460细胞系的增殖。此外，And1 degrader 1主要用于癌症研究领域。

PLD-IN-1（Compound 3r），作为一种有效的磷脂酶D（phospholipase D）抑制剂，其IC50为1.97 μM，能够通过调节肺癌细胞的免疫逃避机制来抑制肿瘤。该化合物能降低CD24、CD47和PD-L1的表达，并增强钙网络蛋白的表达，从而促进巨噬细胞吞噬癌细胞。此外，PLD-IN-1抑制多种肺癌细胞线的细胞活力，包括A549、HCC44、H460和HCC15，其IC50分别为18.44、22.31、24.85和21.45 μM。它还可以诱导A549细胞凋亡（apoptosis）并抑制细胞迁移，同时增强促炎性M1巨噬细胞水平并降低抗炎性M2巨噬细胞水平，展现出在小鼠模型中的抗肿瘤活性。

BCRP-IN-2 是一种BCRP抑制剂，紫外线激活后其抑制效果更显著。BCRP-IN-2 是研究喹唑啉胺衍生物与BCRP相互作用的重要探针，能够促进BCRP转运蛋白的ATP水解，并增加米托蒽醌在BCRP过表达的H460 MX20细胞中的累积。

Microtubulin-IN-1 (Compound 8g) 是一种微管蛋白 (microtubulin) 抑制剂，专门靶向秋水仙碱结合位点，破坏微管蛋白的完整性，并诱导p53蛋白的表达上调。在多种癌细胞系中，Microtubulin-IN-1 展现出抗增殖活性，IC50在NCI-H460、BxPC-3和HT-29中分别为2.4、1.6和2.07 nM。该化合物能在G2/M期阻滞细胞周期，并诱导NCI-H460细胞的凋亡 (apoptosis)。

(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 growth factor beta-activated kinase 1 (TAK1)-inhibitory activities of (5Z)-7-oxozeaenol analogues. Bioorg. Med. Chem. 23(21), 6993-6999 (2015).|2. Ayers, S., Graf, T.N., Adcock, A.F., et al. Resorcylic acid lactones with cytotoxic and NF-κB inhibitory activities and their structure-activity relationships. J. Nat. Prod. 74(5), 1126-1131 (2011).

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 in the H2122 wild-type and nonobese diabetic severe combined immunodeficiency (NOD-SCID) mouse xenograft models when administered at doses of 20 and 6 mg kg, respectively.

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 μg/ml).3

(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.

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 proliferation of PC3 and LNCaP cells (IC50s = 130 and 90 nM, respectively), and induces apoptosis and necrosis in PC3 and LNCaP cells. Malformin A also increases the accumulation of reactive oxygen species, decreases the mitochondrial membrane potential, and induces autophagy in PC3 and LNCaP cells. It is toxic to mice when administered intraperitoneally (LD50 = 3.1 mg/kg) but not orally up to doses of 50 mg/kg.

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 μM, respectively).2 1.Chooi, Y.H., Wang, P., Fang, J., et al.Discovery and characterization of a group of fungal polycyclic polyketide prenyltransferasesJ. Am. Chem. Soc.134(22)9428-9437(2012) 2.Shang, Z., Salim, A.A., Khalil, Z., et al.Viridicatumtoxins: Expanding on a rare tetracycline antibiotic scaffoldJ. Org. Chem.80(24)12501-12508(2015)

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: Antimycobacterial glycosylated polyketide macrolides from the Australian soil Amycolatopsis sp. MST-108494J. Antibiot. (Tokyo)70(12)1097-1103(2017)

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)

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 glycosylated polyketide macrolides from the Australian soil Amycolatopsis sp. MST-108494J. Antibiot. (Tokyo)70(12)1097-1103(2017)

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).

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)