a549 cells

Theophylline monohydrate (Quibron) appears to inhibit phosphodiesterase and prostaglandin production, regulate calcium flux and intracellular calcium distribution, and antagonize adenosine. Theophylline monohydrate is a natural alkaloid derivative of xanthine isolated from the plants Camellia sinensis and Coffea arabica. Physiologically, this agent relaxes the bronchial smooth muscle, produces vasodilation (except in cerebral vessels), stimulates the CNS, stimulates the cardiac muscle, induces diuresis, and increases gastric acid secretion; it may also suppress inflammation and improve contractility of the diaphragm.

Matrine (Vegard), an alkaloid isolated from the Sophora genus, acts as a kappa opioid receptor agonist.

Astragaloside IV (AS-IV), an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1 2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells. Astragaloside IV is a bioactive saponin first isolated from the dried plant roots of the genus Astragalus, which is used in traditional Chinese medicine.1 It dose-dependently inhibits human adenovirus type 3 (HAdV-3) in A549 cells (IC50 = 23 μM; LC50 = 865 μM).It inhibits replication of HAdV-3 and decreases HAdV-3-induced apoptosis. It has diverse protective effects for the cardiovascular, immune, digestive, and nervous systems. In particular, it reduces myocardial infarct size in dogs when administered prior to coronary ligation and reduces reperfusion arrhythmias in isolated rat hearts.

Theophylline (1,3-Dimethylxanthine) is a methyl xanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac, and central nervous system stimulant activities. It inhibits the 3', 5'-cyclic nucleotide phosphodiesterase that degrades cyclic AMP, thus potentiating the actions of agents that act through adenylyl cyclases and cyclic AMP.

H1k is an eudistomin Y fluorescent derivative and lysosome-targeted antiproliferative agent that dose-dependently increases autophagy signalling and down-regulates the expression of cyclin-dependent kinase (CDK1) and cyclin B1.

CLEFMA has anti-proliferative activity. CLEFMA inhibits tumor growth associated with NF-κB-regulated anti-inflammatory and anti-metastatic effects.

OTS186935 FA is a protein methyltransferase SUV39H2 inhibitor.OTS186935 FA inhibits tumor growth in MDA-MB-231 breast cancer cells and A549 lung cancer cells.

HOIPIN-1 (JTP0819958) is a selective and potent inhibitor of linear ubiquitin chain assembly complex (LUBAC) (IC50 >2.8 μM).HOIPIN-1 inhibits LUBAC-mediated NF-kB activation.

MC2590 is a potent and selective histone deacetylase (HDAC) inhibitor that inhibits HDAC1-3, -6, -8, and -10 activities, induces cell cycle arrest, and promotes apoptosis.

ULK1-IN-2 is a potent ULK1 inhibitor with potential anticancer activity, inducing apoptosis while blocking autophagy.ULK1-IN-2 has high cytotoxicity against cancer cells, with an IC50 value of 1.94 μM against A549 cells.ULK1-IN-2 can be used for the study of non-small-cell lung cancer.

OTUB1 USP8-IN-1 is a potent OTUB1 USP8 inhibitor with potential anticancer activity, demonstrating IC50 values of 0.17 nM for OTUB1 and 0.28 nM for USP8. OTUB1 USP8-IN-1 can be used in the study of non-small-cell lung cancer.

Cucurbitacin B (Cuc B) has profound in vitro and in vivo antiproliferative effects against human pancreatic Y cells. It inhibited AKT signaling activation through up-regulation of PTEN. Cucurbitacin B is an effective inhibitor of HIF-1 and provide new perspectives into the mechanism of its anticancer activity. Cucurbitacin B inhibits proliferation and induces apoptosis via STAT3 pathway inhibition in A549 lung Y cells.

NAE-IN-M22 (NEDD8 inhibitor M22) is a selective, potent and reversible inhibitor of NEDD8 activating enzyme (NAE). NAE-IN-M22 inhibits multiple cancer cell lines and induces apoptosis in A549 cells. NAE-IN-M22 also can inhibit tumor growth in vivo.

Lawsone methyl ether (2-Methoxy-1,4-naphthoquinone) induces apoptosis in A549 cells independently of cell cycle arrest, mediated by JNK and p38 MAPK signaling pathways. These pathways are activated due to oxidative DNA damage from increased ROS generation in MNQ-treated A549 cells.

Inauhzin (INZ)(INZ) is a novel small molecule that effectively reactivates p53 by inhibiting SIRT1 activity, promotes p53-dependent apoptosis of human Y cells without causing apparently genotoxic stress(IC50=3 uM, in A549 cell).

Sphondin has anticonvulsant, anti-inflammatory, and anti-proliferative activities, it possessed an inhibitory effect on IL-1beta-induced increase in the level of COX-2 protein and PGE(2) release in A549 cells.

WZB117 is a Glucose Transporter 1 (GLUT1) inhibitor. when IC50 of WZB117 approximate 10 μM, it inhibits lung cancer A549 cells and breast cancer MCF7 cells proliferation.

GW-870086 is an effective anti-inflammatory agent. GW-870086 also plays a role in a glucocorticoid receptor agonist (pIC50: 10.1 in A549 cells expressing NF-κB).

Myrislignan has anti-inflammatory, and anti-cancer activities, it inhibited NF-κB signalling pathway activation, inhibited the proliferation of A549 cells in a dose- and time-dependent manner, it also significantly induced apoptosis and cell cycle arrest

AEM1 is an inhibitor of deregulated NRF2 transcriptional activity in cancer. AEM1 acts by broadly decreasing the expression of NRF2 controlled genes, sensitizing A549 cells to various chemotherapeutic agents, and inhibiting the growth of A549 cells in vitro and in vivo.

MDK-7933 (HDAC8-IN-1) is a HDAC8 inhibitor with an IC50 of 27.2 nM in cancer cell lines. MDK-7933 shows antiproliferative effects toward several human lung cancer cell lines (A549, H1299, and CL1-5). HDAC8-IN-1 exhibits cytotoxicity against human lung CL1-5 cells without significant cytotoxicity for normal IMR-90 cells[1].

2,5-dimethyl Celecoxib is a derivative of celecoxib that does not inhibit COX-2 (IC50 = >100 μM).1 It does inhibit microsomal prostaglandin E synthase-1 (mPGES-1) in HeLa cells (IC50 = 15.6 μM) and reduces prostaglandin E2 production in HeLa, A549, and HCA-7 cells (IC50s = 0.64, 0.83, and 3.08 μM, respectively).2 It inhibits proliferation of drug-sensitive RPMI8226 and multidrug-resistant 8226 Dox40 multiple myeloma cells, as well as increases the rate of apoptosis when used at concentrations of 20 and 30 μM.3 2,5-dimethyl Celecoxib reduces the expression of survivin, cyclin A, cyclin B, MEK1, and MEK2 in 8226 Dox40 cells. The antiproliferative effect of 2,5-dimethyl celecoxib is independent of mPGES-1 inhibition.2References1. Zhu, J., Song, X., Lin, H.-P., et al. Using cyclooxygenase-2 inhibitors as molecular platforms to develop a new class of apoptosis-inducing agents. J. Natl. Cancer Inst. 94(23), 1745-1757 (2002).2. Wobst, I., Schiffmann, S., Birod, K., et al. Dimethylcelecoxib inhibits prostaglandin E2 production. Biochem. Pharmacol. 76(1), 62-69 (2008).3. Kardosh, A., Soriano, N., Liu, Y.-T., et al. Multitarget inhibition of drug-resistant multiple myeloma cell lines by dimethyl-celecoxib (DMC), a non-COX-2 inhibitory analog of celecoxib. Blood 106(13), 4330-4338 (2005). 2,5-dimethyl Celecoxib is a derivative of celecoxib that does not inhibit COX-2 (IC50 = >100 μM).1 It does inhibit microsomal prostaglandin E synthase-1 (mPGES-1) in HeLa cells (IC50 = 15.6 μM) and reduces prostaglandin E2 production in HeLa, A549, and HCA-7 cells (IC50s = 0.64, 0.83, and 3.08 μM, respectively).2 It inhibits proliferation of drug-sensitive RPMI8226 and multidrug-resistant 8226 Dox40 multiple myeloma cells, as well as increases the rate of apoptosis when used at concentrations of 20 and 30 μM.3 2,5-dimethyl Celecoxib reduces the expression of survivin, cyclin A, cyclin B, MEK1, and MEK2 in 8226 Dox40 cells. The antiproliferative effect of 2,5-dimethyl celecoxib is independent of mPGES-1 inhibition.2 References1. Zhu, J., Song, X., Lin, H.-P., et al. Using cyclooxygenase-2 inhibitors as molecular platforms to develop a new class of apoptosis-inducing agents. J. Natl. Cancer Inst. 94(23), 1745-1757 (2002).2. Wobst, I., Schiffmann, S., Birod, K., et al. Dimethylcelecoxib inhibits prostaglandin E2 production. Biochem. Pharmacol. 76(1), 62-69 (2008).3. Kardosh, A., Soriano, N., Liu, Y.-T., et al. Multitarget inhibition of drug-resistant multiple myeloma cell lines by dimethyl-celecoxib (DMC), a non-COX-2 inhibitory analog of celecoxib. Blood 106(13), 4330-4338 (2005).

Cnidicin has anti-allergic and anti-inflammatory activity, it inhibits the degranulation of mast cell and the NO generation in RAW 264.7 cells(IC50 value, 7.5 microM). Cnidicin exhibits a significant inhibition on the proliferation of cultured human tumor

PARP1-IN-8 (N-(3-chlorophenyl)-3-(1-oxo-4-phenylphthalazin-2(1H)-yl)propanamide) is an effective inhibito of PARP1 (IC50 = 97 nM).

M2N12 is a potent and highly selective inhibitor of cell division cycle 25C protein phosphatase (Cdc25C, IC50 = 0.09 μM) and also exhibits anti-tumor activity. Additionally, M2N12 shows promising activity against Cdc25A (IC50 = 0.53 μM) and Cdc25B (IC50 = 1.39 μM).

GPNA hydrochloride is specific glutamine (Gln) transporter ASCT2(SLC1A5) inhibitor. GPNA reversibly induces apoptosis in A549 cells. GPNA hydrochloride is a well-known substrate of the enzyme γ-glutamyltransferase (GGT). GPNA hydrochloride also inhibits

8-Chloroadenosine (NSC-354258) is a 5' AMP-activated protein kinase agonist potentially for the treatment of chronic lymphocytic leukemia. 8-chloroadenosine activity is associated with inhibition of the mTOR pathway.8-Chloroadenosine (NSC-354258) is a nucleoside analog; metabolized in vivo to 8-Chloro-ATP. Incorporates into RNA during transcription and inhibits RNA synthesis. Exhibits cytotoxicity in MM.1S, RPMI-8226, and U266 cancer cell lines; induces G2/M cell cycle arrest and mitotic catastrophe in A549 and H1299 cells. 8-Chloroadenosine (NSC-354258) has been shown to deplete ATP and inhibit tumor growth in hematological malignancies as well as in lung and breast cancer cell lines.

NF-κB-IN-1 (1,6-Heptadiene-3,5-dione, 1,7-bis(3,4-dimethoxyphenyl)-4-[(4-hydroxy-3-methoxyphenyl)methylene]-, (1E,6E)-) is a potent NF-κB signaling pathway inhibitor. It is a 4-arylidene crucumin analogue. NF-κB-IN-1 directly inhibits IKK to block NF-κB activation. NF-κB-IN-1 effectively inhibits the viability of lung cancer cells and attenuates the clonogenic activity of A549 cells.

PF-6274484, a high affinity, irreversible covalent inhibitor of EGFR kinase with Ki of 0.14 nM, inhibits the autophosphorylation of wild-type EGFR in A549 cells and EGFRL858R/T790M in H1975 cells with IC50 of 5.8 nM and 6.6 nM, respectively.

Myrothecine A, a trichothecene mycotoxin discovered in M. roridum, exhibits anticancer properties. It effectively inhibits the proliferation of various cancer cell lines, specifically A549, MCF-7, HepG2, and SMMC-7721, with IC50 values of 95, 70, 60, and 25 µM, respectively. At a concentration of 50 µM, Myrothecine A induces G1 cell cycle arrest in HepG2 cells and promotes apoptosis in SMMC-7721 cells by elevating levels of Bax and cleaved caspase-3, -5, and -8.

1beta-Hydroxytorilin exhibits cytotoxicity against human A549, SK-OV-3, SK-MEL-2, and HCT15 tumor cells.

(E)-2-(2-Chlorostyryl)-3,5,6-trimethylpyrazine (CSTMP) is a stilbene derivative with antioxidant and anticancer activities. It stimulates proliferation of hydrogen peroxide-damaged ECV-304 cells (EC50 = 24.9 nM). CSTMP reduces hydrogen peroxide-induced release of lactate dehydrogenase (LDH) in and increases viability of human umbilical vein endothelial cells (HUVECs) in a concentration-dependent manner via inhibition of apoptosis. It reverses hydrogen peroxide-induced release of malondialdehyde (MDA) and decreases in superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) activities as well as increases constitutive nitric oxide synthase (cNOS) activity and nitric oxide (NO) production in HUVECs. CSTMP also induces cell death of A549 non-small cell lung cancer (NSCLC) cells in an IRE1α-dependent manner through induction of IRE1α-TRAF2-ASK1 complex-mediated endoplasmic reticulum (ER) stress and mitochondrial apoptosis.

AZD-3409 is a potent prenyl transferase inhibitor. AZD-3409 showed higher potency than lonafarnib. The mean IC(50) for cytotoxicity of AZD3409 was 510 in MEF cells, 10,600 in A549 cells and 6,170 in MCF7 cells, respectively. In these cells, the IC(50) for FTase activity of AZD3409 ranged from 3.0 to 14.2 nM and of lonafarnib from 0.26 to 31.3 nM. AZD3409 inhibits farnesylation to a higher extent than geranylgeranylation. Both inhibition of farnesylation and geranylgeranylation could not be correlated to the antiproliferative activity of the drug. AZD3409 might be active in gefitinib-resistant breast carcinoma.

CAY10763 is a dual inhibitor of indolamine 2,3-dioxygenase 1 (IDO1; IC50= 46 nM) and STAT3 activation.1It binds to STAT3 (Kd= 530 nM) and selectively reduces the levels of STAT3 phosphorylated at the tyrosine in position 705 (STAT3Y705) over phosphorylated STAT3S727, STAT1, and STAT5 in SKOV3 cells when used at a concentration of 500 nM. It also inhibits STAT3 nuclear translocation in SKOV3 cells. CAY10763 is cytotoxic to HCT116, SKOV3, A549, and HepG2 cancer cells (IC50s = 37, 28, 33, and 12 nM, respectively). It reduces tumor growth in B16/F10 mouse melanoma and HepG2 mouse xenograft models when administered at doses of 100 and 10 mg/kg, respectively. 1.Huang, R., Jing, X., Huang, X., et al.Bifunctional naphthoquinone aromatic amide-oxime derivatives exert combined immunotherapeutic and antitumor effects through simultaneous targeting of indoleamine-2,3-dioxygenase and signal transducer and activator of transcription 3J. Med. Chem.63(4)1544-1563(2020)

Neoaureothin, a bacterial metabolite found in Streptomyces, is an androgen receptor (AR) antagonist that inhibits dihydrotestosterone (DHT) binding to ARs (IC50 = 13 μM) and DHT-induced prostate-specific antigen expression in LNCaP cells (IC50 = 1.75 nM). It is cytotoxic to A549, HCT116, and HepG2 cells (IC50s = 34.3, 47, and 37.2 μg ml, respectively), exhibits nematocidal activity against the pine wood nematode B. xylophilus (LC50 = 0.84 μg ml), and increases survival of P. densiflora trees inoculated with B. xylophilus.

Antitumor agent-112 (compound 3a) is a potent antitumor compound that induces apoptosis and exhibits cytotoxic activity on A549 cells, with an IC50 value of 91.35 μM [1].

Beta-Tocotrienol to serve as a new anticancer agent for treating human lung and brain cancers. It inhibits the growth of both A549 (GI50=1.38±0.334μM) and U87MG (GI50=2.53±0.604μM) cells at rather low concentrations.

LSD1-IN-14, a powerful and specific inhibitor of LSD1 (with an IC50 value of 0.89 μM), effectively suppresses the growth of A549 and THP-1 cells and promotes the apoptosis of tumor cells [1].

KRAS inhibitor-14 is a potent inhibitor of KRAS G12C (IC50: 0.249 μM). KRAS inhibitor-14 exhibited p-ERK inhibition in MIA PaCA-2, A549 cells with IC50s of 1.12, >33.3 μM, respectively. KRAS inhibitor-14 has potential to be investigated in pancreatic, colorectal and lung cancers.

Antitumor agent-60 is a potent antitumor agent that targets the RAS-RAF signaling pathway and binds to CRAF (Kd: 721.3 nM). antitumor agent-60 increases p53 and ROS levels in cancer cells, resulting in oval and irregular nuclei. antitumor agent-60 is sufficient to block the cell cycle in G2/M phase and induce apoptosis. Antitumor agent-60 is sufficient to block the cell cycle in G2/M phase and induce apoptosis. In the A549 tumor transplantation model, Antitumor agent-60 has the ability to inhibit tumor growth.

DL-Alanine (DL-2-Aminopropionic acid) is an amino acid that is a racemic compound of L- and D-alanine.DL-Alanine is often used as a reducing and capping agent in conjunction with aqueous silver nitrate for nanoparticle generation.DL-Alanine is a sweetening agent, and can be grouped with glycine and sodium saccharin.DL-Alanine plays an important role in glucose-alanine cycling between tissues and liver.DL-Alanine can be used to study the chelation of transition metals such as Cu, Zn, and Cd. DL-Alanine plays an important role in the glucose-alanine cycle between tissues and the liver.DL-Alanine can be used to study the chelation of transition metals such as Cu, Zn, and Cd.

Edgeworin is a DNA polymerase beta (pol beta) inhibitor, it inhibits both the lyase and polymerase activities of DNA polymerase beta; it can potentiate the inhibitory action of the anticancer drug bleomycin in cultured A549 cells via an inhibition of DNA

Anticancer agent 59, an inhibitor active against various cancer cell lines, particularly demonstrates efficacy in A549 cells with an IC 50 value of 0.2 μM. It prompts apoptosis, elevates Ca2+ and ROS levels within cancer cells, and markedly reduces mitochondrial membrane potential. Additionally, it effectively curtails tumor growth in the A549 mouse xenograft model.

SARS-CoV-2 Mpro-IN-5 is a dual inhibitor targeting Main Protease (M Pro) and Cathepsin L (CatL) with IC50 values of 1800 nM and 145 nM, respectively. This compound demonstrates antiviral activity by inhibiting SARS-CoV-2 replication in hACE2 expressing A549 cells, with an IC50 value of 14.7 nM.

CPT-Se3, a camptothecin (CPT) seleno-derivative, exhibits enhanced anticancer efficacy by effectively killing cancer cells and hindering tumor proliferation. This compound diminishes the GSH/GSSG ratio and total thiols while increasing ROS levels, ultimately triggering apoptosis in Hep G2 cells. Furthermore, CPT-Se3 demonstrates significant cytotoxicity against HeLa, Hep G2, A549, and SMMC-7721 cell lines with IC50 values ranging from 2.19 to 4.7 μM [1].

TC113, a Gemcitabine (GEM)-based conjugate incorporating the c(RGDyK) sequence, is internalized by A549 cells via the integrin αvβ3 pathway. It demonstrates significant antiproliferative effects on both WM266.4 and A549 cell lines.

TP0427736 hydrochloride can be used in the androgenic alopecia (AGA) research. TP0427736 hydrochloride inhibits the phosphorylation of Smad2/3 in A549 cells induced by TGF-β1 with an IC50 value of 8.68 nM. TP0427736 hydrochloride is a potent ALK5 kinase inhibitor with an IC50 value of 2.72 nM which is 300-fold more potent than inhibitory effect against ALK3 of 836 nM [1].

T-Type calcium channel inhibitor 2 (compound 6g) is a potent inhibitor of the T-type calcium channel, specifically acting on Cav3.1 (α1G) with an IC50 of 31.0 μM, Cav3.2 (α1H) with an IC50 of 83.1 μM, and Cav3.3 (α1I) (α1H). T-Type calcium channel inhibitor 2 exhibited cytotoxicity against A549 and HCT-116 cells with IC50s of 5.0 μM and 6.4 μM, respectively.

Ansatrienin B is an ansamycin antibiotic and antifungal agent first isolated from S. collinus and S. rishiriensis., In fetal rat long bones, it is an inhibitor of parathyroid hormone-induced calcium release (IC50 = 21 nM), which is a measure of bone resorption, and pp60c-src kinase (IC50 = 50 nM). It is an inhibitor of translation at the protein synthesis stage by specific inhibition of L-leucine incorporation (IC50 = 58 nM in A549 cells). It also inhibits TNF-α-induced expression of intercellular adhesion molecule-1 (ICAM-1; IC50 = 300 nM). Early in vitro studies showed that ansatrienin B potentiates the chemotherapeutic action of 5-fluorouracil , cisplatin , bleomycin , mitomycin C , and 6-mercaptopurine. Ansatrienin B is a hydroquinone form of ansatrienin A .

ARN24139 is a topoisomerase II poison (IC50= 7.3 μM in a topoisomerase II decatenation assay).1It inhibits proliferation of DU145, HeLa, and A549 cells (IC50s = 4.7, 3.8, and 3.1 μM, respectively). 1.Arencibia, J.M., Brindani, N., Franco-Ulloa, S., et al.Design, synthesis, dynamic docking, biochemical characterization, and in vivo pharmacokinetics studies of novel topoisomerase II poisons with promising antiproliferative activityJ. Med. Chem.63(7)3508-3521(2020)

HT-2 Toxin, a deacetylated metabolite of T-2 toxin, impairs protein synthesis and hinders cell proliferation in plants.