lung adenocarcinoma

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

Silibinin (Silybin) is the major active constituent of silymarin, a standardized extract of the milk thistle seeds, containing a mixture of flavonolignans consisting of silibinin, isosilibinin, silicristin, silidianin and others. Silibinin itself is a mixture of two diastereomers, silybin A and silybin B, in approximately equimolar ratio. Both in vitro and animal research suggest that silibinin has hepatoprotective (antihepatotoxic) properties that protect liver cells against toxins. Silibinin has also demonstrated in vitro anti-cancer effects against human prostate adenocarcinoma cells, estrogen-dependent and -independent human breast carcinoma cells, human ectocervical carcinoma cells, human colon cancer cells, and both small and nonsmall human lung carcinoma cells.

SMIFH2 is formin homology 2 (FH2) domains inhibitor.

Brigimadlin (BI 907828) is an orally active and highly potent E3 ubiquitin-protein ligase MDM2-p53 antagonist with antitumor activity.Brigimadlin can be used to study metastatic BTC, PDAC, lung adenocarcinoma, or bladder cancer.

PARP-1-IN-2 is a potent PARP1 inhibitor that crosses the blood-brain barrier (IC50: 149 nM).PARP-1-IN-2 showed significant antiproliferative activity against the human lung adenocarcinoma epithelial cell line A549 in cellular assays.PARP-1-IN-2 induced apoptosis in A549 cells.

BPI-9016M is an effective, orally active, and selective dual inhibitor of c-Met and AXL tyrosine kinases. It suppresses tumor cell growth, invasion, and migration of lung adenocarcinoma.

KY-05009 is a chemical compound that effectively suppresses TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in human lung adenocarcinoma cells, reduces TNIK protein expression and the transcriptional activity of Wnt target genes, and promotes apoptosis in cancer cells, displaying anti-cancer properties. Furthermore, it functions as an ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with a Ki of 100 nM.

GSK319347A is a selective and potent dual inhibitor of TBK1 and IKKε with potential anti-tumor activity and inhibition of IKK2 activity, which can be used in the study of bladder cancer and lung adenocarcinoma.

PARP1-IN-31 (compound 11f), a thiazolopyridone-based compound, exhibits potent inhibition against PARP-1, with an IC50 value of 97 nM. It acts as an anti-lung adenocarcinoma agent, capable of inducing apoptosis and inhibiting cell proliferation in lung cancer cell lines.

UNBS3157 is a novel naphthalimide derivative that is non-hematotoxic and exhibits significant antitumor activity through DNA intercalation and the poisoning of topoisomerase IIalpha. Unlike Amonafide, a related naphthalimide compound that showed activity in Phase II breast cancer trials but did not proceed to Phase III due to dose-limiting myelotoxicity, UNBS3157 has a maximum tolerated dose 3-4 times higher and does not cause hematotoxicity in mice at effective antitumor doses. In vivo models, including (i) L1210 mouse leukemia, (ii) MXT-HI mouse mammary adenocarcinoma, and (iii) human A549 non-small cell lung carcinoma and BxPC3 pancreatic cancer orthotopic models, demonstrate superior efficacy of UNBS3157 compared to Amonafide.

SBI-183 is an orally active QSOX1 inhibitor (Kd: 20 μM). It can inhibit the proliferation and invasion phenotypes of renal carcinoma cell lines, triple-negative breast cancer cell lines, lung adenocarcinoma cell lines, and pancreatic ductal adenocarcinoma. In vivo, SBI-183 suppresses tumor growth in two human renal cell carcinoma xenograft mouse models.

CDK2/FLT4/PDGFRA-IN-1 (Compound 4a) is a potent inhibitor of CDK2/cyclin A, FLT4 (VEGFR3), and PDGFRA, with IC50 values of 1.672, 0.554, and 0.629 μM respectively. This compound demonstrates significant antiproliferative effects on cancer cells, including lung cancer EBC-1, pancreatic ductal adenocarcinoma AsPC-1, and colorectal cancer HT-29 cells. Additionally, CDK2/FLT4/PDGFRA-IN-1 can induce apoptosis in these cancer cells.

PKM2-IN-10 is a PKM2 inhibitor. It effectively suppresses the proliferation of A549 and HCC1833 cell lines with IC50 values of 3.36 μM and 9.20 μM, respectively. PKM2-IN-10 demonstrates antitumor activity in human non-small cell lung cancer (NSCLC) and mouse lung adenocarcinoma models. It is applicable for research in lung cancer.

Nemadipine A is an L-type calcium channel blocker that induces morphological and growth defects in wild-type C. elegans and those with hypoexpression of egl-19, which encodes the only L-type calcium channel α1-subunit in the C. elegans genome. It also inhibits L-type calcium channels in chick ciliary neurons. Nemadipine A increases TRAIL-induced cytotoxicity and synergistically enhances caspase-8 and caspase-3 activation in a concentration-dependent manner in H1299 lung adenocarcinoma cells. It also decreases Survivin expression when used alone or in combination with TRAIL in A549 cells.

Chromomycin A2 is an aureolic acid that has been found in several marine actinomycetes and has antibacterial and anticancer activities. Chromomycin A2 inhibits the growth of B. subtilis in an agar diffusion assay. It also inhibits the growth of human SGC7901 gastric cancer, HepG2 hepatocellular carcinoma, A549 lung epithelial adenocarcinoma, HCT116 colon cancer, and COC1 ovarian cancer cells, as well as human umbilical vein endothelial cells (HUVECs; IC50s = 4, 0.5, 3, 5, 5, and 8 nM, respectively). Chromomycin A2 (30 nM) halts the cell cycle in the G0 G1 phase and increases the protein levels of LC3A and LC3B in MALME-3M melanoma cells, indicating that it induces autophagy. It also increases the levels and promoter activity of the autophagic proteins ATG7 and ATG10 and reduces cell viability to 50% in human SCC-11 squamous cell carcinoma cells when used at a concentration of 30 nM.

Chrysomycin B is an antibiotic isolated from *Streptomyces* sp. that induces DNA damage and inhibits topoisomerase II in the human lung adenocarcinoma (A549) cell line.

LCS3 is a reversible and non-competitive synergistic inhibitor of glutathione disulfide reductase (GSR) and thioredoxin reductase 1 (TXNRD1) with IC50s of 3.3 μM and 3.8 μM, respectively. LCS3 has antitumour activity, induces apoptosis and can be used in the study of lung adenocarcinoma (LUAD).

Antitumor agent-44 (Compound 5n) elicits potent antitumor effects by disrupting mitochondrial homeostasis, inducing cell cycle arrest, and triggering apoptosis in human adenocarcinoma cells. Additionally, Antitumor agent-44 demonstrates significant anti-tumor activity in a lung cancer cell xenograft mice model [1].

Antitumor agent-75 is a novel and potent antitumor agent with cytotoxic effects on both cancer and normal human cell lines. In combination with antitumor agent-74, Antitumor agent-75 exhibits a highly selective cytotoxic effect (IC50: 2.8 μM) against human lung adenocarcinoma [cell line A549]. Antitumor agent-75 is applicable in cancer research.

IST-622 is a unique topoisomerase inhibitor, showing significant growth-inhibitory effects against large-cell lung cancer (Lu-116) and gastric adenocarcinoma (St-4).

Nidanilimab (CAN04) is a fully humanized IL1RAP monoclonal antibody with a Kd value of 1.10 pM. It exhibits antitumor activity by disrupting the IL1α and IL1β signaling pathways and inducing the immune system to destroy tumor cells. Nidanilimab can be used to study solid cancers, such as non-small cell lung cancer (NSCLC) and pancreatic ductal adenocarcinoma (PDAC).

Inetetamab is a humanized monoclonal antibody targeting HER2 receptor domain IV, exhibiting antitumor activity through inducing pyroptosis in lung adenocarcinoma. It is used in studies of HER2-positive metastatic breast cancer.

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].

Pixinol, a natural glycoside, demonstrates cytotoxic effects on human lung carcinoma GLC4 and adenocarcinoma COLO 320 cell lines with IC50 values of 71 µM and 43 µM, respectively [1].