h460

Tubulin inhibitor 8 is an inhibitor of tubulin and various cancer cell lines and inhibits tubulin polymerisation and K562 cell growth with an IC50 of 0.73 μM and 14 nM respectively.

PSB-15160 is a compound that inhibits the growth of MCF7 (breast), NCI-H460 (lung) and SF-268 (NCS) cells in the treatment of estrogen-dependent tumours.

RHPS4 (RHPS 4 methosulfate) is a potent inhibitor of Telomerase at submicromolar.

IACS-010759 is an orally bioavailable inhibitor of complex I of oxidative phosphorylation of the mitochondrial electron transport chain.

Volasertib (BI 6727) (BI-6727) is a potent inhibitor of PLK1 (IC50: 0.87 nM), inducing mitotic arrest and apoptosis. It also inhibits PLK2/PLK3 (IC50s: 5/56 nM).

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)

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)

Ros-generating agent 1 has anticancer activity and generates ROS by covalently modifying Sec-498 residues of TrxR. ROS-generating agent 1 reduces intracellular TrxR protein levels and promotes ROs-dependent apoptosis and ferroptosis in NCI-H460 cells.

Sartorypyrone B, a 2β-acetoxyl analogue of chevalone C, is derived from the ethyl acetate extract of the culture of Neosartorya tsunodae (KUFC 9213), a fungus associated with marine sponges. This compound demonstrates potent growth inhibitory activity against MCF-7, NCI-H460, and A375-C5 cancer cell lines with GI50 values of 17.8, 20.5, and 25.0 μM, respectively, indicating its potential in the study of breast adenocarcinoma, non-small cell lung cancer, and melanoma [1].

Antitumor Agent-105 (Compound 37) exhibits antitumor activity, demonstrating inhibition of A549, H1299, H460, HCT116, and MDA-MB-231 cells with respective IC50 values of 6.7, 8.3, 4.3, 4.4, and 6.7 μM [1].

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

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)

Norartocarpetin is a potent tyrosinase inhibitor exhibiting significant antibrowning properties useful for food system research, with an IC50 of 0.47 μM. Furthermore, it demonstrates substantial anticancer activity specifically in lung carcinoma cells (NCI-H460), achieving an IC50 of 22 μM. The antiproliferative effects of Norartocarpetin are achieved through targeting the Ras/Raf/MAPK signaling pathway, inducing mitochondrial-mediated apoptosis, facilitating S-phase cell cycle arrest, and inhibiting cell migration and invasion in human lung carcinoma cells.

CP-640186 is an isozyme-nonselective Acetyl-CoA carboxylase (ACCase) inhibitor. The IC50s of CP-640186(CP 640186) is 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively.

Ilorasertib (ABT-348) (ABT-348) is an ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora A/Aurora B/Aurora C (IC50s: 120 nM/7 nM/1 nM). It also suppresses RET tyrosine kinase, PDGFRβ, and Flt1 (IC50s: 7 nM, 3 nM, and 32 nM).

(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).

Antiproliferative agent-6 (compound 8a) is a potent antitumor compound. Antiproliferative agent-6 shows antiproliferative activity. Antiproliferative agent-6 inhibits cancer cell lines HCT116, MCF-7, H460 and non-tumor aneuploid immortal keratinocyte HaCaT cells with GI 50 s of 0.5 μM, 2 μM, 0.7 μM and 3.5 μM, respectively.

Compounds 17o (IC50: 14.0 nM, NCI-H460) and 17p (IC50: 2.9 nM, NCI-H460) with furan moieties showed potent cytotoxic effects at the nanomolar level against various human cancer cell lines.

Compound 6h (Anticancer Agent 139) exhibits potent anticancer activity, engaging in a π-cationic interaction with Lys352 of Tubulin and demonstrating high efficacy against SNB-19, OVCAR-8, and NCI-H460 with PGIs of 86.61, 85.26, and 75.99, respectively. Moreover, it shows moderate activity against a range of other cancer cell lines — HOP-62, SNB-75, ACHN, NCI/ADR-RES, 786-O, A549/ATCC, HCT-116, and MDA-MB-231 — with PGIs between 51.88 and 67.55 [1].

HP661, a selective inhibitor of mitochondrial complex I (NADH dehydrogenase), impedes complex I activity by 77.6% at 1 µM, demonstrating lesser inhibition towards complex III (28.1%) and no inhibitory effects on complexes II and IV. It notably decreases the viability of human lung cancer cells—H460, NCI H441, and trametinib-resistant A549 cells (IC50s = 10.6, 29.7, and 15.1 nM, respectively)—which exhibit high levels of oxidative phosphorylation. In contrast, it shows minimal activity against NCI H358 lung cancer cells and non-cancerous HPNE and MRC-5 cells (IC50s = >10,000 nM for both), which have lower oxidative phosphorylation levels. Furthermore, in an H460 mouse xenograft model, HP661 at a dose of 30 mg/kg twice daily significantly reduces tumor volume and enhances the tumor-growth inhibitory effects of trametinib.

PD 0332991, an unsymmetrical indolocarbazole compound, is cell-permeable and exhibits antiproliferative effects by functioning as a potent, selective, reversible, and ATP-competitive inhibitor of Cdk4/D1 (IC 50 = 76 nM). Although it can inhibit other Cdks, such as Cdk2/E and Cdk1/B, effectiveness requires higher concentrations (IC 50 = 520 nM and 2.1 µM, respectively) and demonstrates minimal activity against CaMKII, PKA, or GSK-3β (IC 50 ≥ 12.4 µM). PD 0332991 efficiently inhibits tumor cell growth in HCT-116 and NCI-H460 cell lines with an IC 50 < 3.0 µM, primarily through blocking Rb phosphorylation and inducing G1 cell cycle arrest.

NSD3-IN-2, a potent inhibitor of NSD3, exhibits an IC50 value of 17.97 μM. It effectively inhibits the growth and proliferation of non-small cell lung cancer (NSCLC) cell lines, including H460, H1299, and H1650, demonstrating significant anticancer activity.

Sodium aurothiomalate is a gold compound that is used for its immunosuppressive anti-rheumatic effects. Aurothiomalate sodium (Miochrysin) is a potent and selective inhibitor of oncogenic PKC-ι signaling. Aurothiomalate sodium is a potent thioredoxin reductase (TrxR) inhibitor. Aurothiomalate sodium exhibits potent anti-tumor activity.

Gypsogenin (639-14-5) is a naturally occurring biochemical that shows anti-ABL1 kinase and anti-chronic Myelogenous Leukemia activities.

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.

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].

Microtubule inhibitor 4 (compound 2) is a potent inhibitor of microtubule and inhibits microtubule protein polymerization, HT-29 cells (IC50: 2.1 nM) exhibited cytotoxicity.

WES-1 (Compound 8g), a carbonic anhydrase IX inhibitor (Ki: 55.9 μM), exhibits broad-spectrum antiproliferative activity against various cancer cell lines, including leukemia (K-562 and MOLT-4), non-small cell lung cancer (NCI-H460), colon cancer (HCT 116 and HCT-15), and melanoma (LOX IMVI) [1].

CVT-11127 is an StearoylCoA Desaturase-1 (SCD1) inhibitor.

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

Compounds 17o (IC50= 14.0 nM, NCI-H460) and 17p (IC50= 2.9 nM, NCI-H460) with furan moieties show potent nanomolar levels of cytotoxic activity against various human cancer cell lines.

(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.

NSD3-IN-3, a potent inhibitor of NSD3, demonstrates significant anticancer activity by inhibiting the growth and proliferation of the non-small cell lung cancer cell line H460, with an IC50 value of 1.86 μM.

Microtubule inhibitor 6 (compound 17o) is a potent microtubule inhibitor. microtubule inhibitor 6 exhibited cytotoxicity against NCI-H460 cells, BxPC-3 cells, and HT-29 cells, with IC50 values of 14.0, 6.6, and 7.0 nM, respectively. Microtubule inhibitor 6 was able to effectively inhibit microtubule polymerization.

HS-243 is an inhibitor of IRAK-4 and IRAK-1 with IC50s of 20 and 24 nM. HS-243 shows anti-inflammatory and anticancer activity.

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)

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.

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.

CP-640186 hydrochloride (CP 640186 HCl) is an isozyme-nonselective acetyl-CoA carboxylase (ACC) inhibitor, including rat liver ACC1 (IC50: 53 nM) and rat skeletal muscle ACC2 (IC50: 61 nM); with higher metabolic stability than CP-610431.

33-BCRP inhibitor is a compound that blocks the action of breast cancer resistance protein (BCRP), enhancing the susceptibility of mitoxantrone-resistant H460/MX20 lung cancer cells to the cytotoxic effects of mitoxantrone, both individually and when combined with UV radiation. Additionally, it enhances the sensitivity of KB-C2 epidermal carcinoma cells, which overexpress P-glycoprotein (P-gp) or multidrug resistance protein (MDR), to colchicine-induced apoptosis. Furthermore, at a concentration of 5 µM, it boosts the intracellular accumulation of mitoxantrone in H460/MX20 cells.

DNA crosslinker 2 (dihydrochloride) is a potent minor groove binder exhibiting a Δ T m of 1.2 °C, indicative of its DNA binding affinity. This compound demonstrates inhibitory activity against cancer cell lines NCI-H460, A2780, and MCF-7, making it applicable for anticancer research [1].

DNA Crosslinker 4 (dihydrochloride) is a potent binder of the DNA minor groove with inhibitory effects on cancer cell lines NCI-H460, A2780, and MCF-7. It is utilized in research for anticancer applications [1].

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)

Sertindole (Lu 23-174) is an atypical antipsychotic that binds to dopamine D2 receptors and the serotonin (5-HT) receptor subtypes 5-HT1D, 5-HT2A, and 5-HT2C (Kds = 2.7, 20, 0.14, and 6 nM, respectively)

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.

17(R)-Resolvin D3 (17(R)-RvD3) is an aspirin-triggered epimer of resolvin D3, produced from docosahexaenoic acid (DHA) through the action of COX-2 in the presence of aspirin, via a 17(R)-hydroperoxy DHA (17(R)-HDHA) intermediary. Identified in mouse inflammatory exudates, 17(R)-RvD3 notably inhibits the transmigration of isolated human polymorphonuclear cells (PMNs) and fosters the efferocytosis of apoptotic PMNs by macrophages. Furthermore, in a mouse model of zymosan-induced peritonitis, 17(R)-RvD3 administration (10 ng/animal) significantly curtails neutrophil infiltration into the peritoneal cavity and modulates cytokine levels by reducing IL-6 and increasing IL-10 in the inflammatory exudate. It engages GPR32, evidenced by activation in a β-arrestin reporter assay and augments phagocytosis more effectively in CHO cells overexpressing GPR32 compared to controls. Additionally, 17(R)-RvD3 enhances the clearance of etoposide-induced tumor cell debris by monocyte-derived macrophages in H460 human lung carcinoma.

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).

Elinafide, a dinaphthylimide cytotoxic agent, is a DNA-targeted anticancer agent that has shown antitumor activity in in vitro and in vivo assays.

c-Met-IN-10 is a potent c-Met kinase inhibitor (IC50: 16 nM). c-Met-IN-10 inhibits the activity of cancer cells A549, H460 and HT-29, and inhibits A549 cell movement by inhibiting HT-29 cell colony formation, which in turn induces apoptosis in HT-29 and A549 cells. c-Met-IN-10 can be used in anticancer studies. -Met-IN-10 is capable of being used in anticancer studies.

Anticancer agent 16 showed good cytotoxic effects on HCT-116 cell line (IC50: 8.55 μM), NCI-H460 cell line (IC50: 5.41 μM) and SKOV3 cell line (IC50: 6.4 μM).