non-small cell lung cancer cell line

Olomoucine is an ATP-competitive inhibitor of Cdk2/cyclin A, Cdc2/CyclinB, CDK2/CyclinE, CDK5/p35, and ERK1/p44 MAP kinase with IC50s of 7, 7, 7, 3, and 25 µM, respectively. It regulates the cell cycle and exhibits anti-melanin tumor activities.

FJ9 is an effective Wnt/β-catenin antagonist (Ki = 29 μM) that downregulates canonical Wnt signaling, inhibits HSC (hepatic stellate cell) activation, and reduces MeCP2 protein levels. FJ9 also disrupts the protein-protein interaction between Frz7 and the DVL PDZ domain, induces apoptosis in human cancer cell lines, and inhibits tumor growth in a mouse xenograft model.

EGFR-IN-150 is an EGFR inhibitor that effectively inhibits the phosphorylation of mutant epidermal growth factor receptor (EGFR) and its downstream AKT signaling pathway, exerting antitumor effects and inducing HMOX1 expression to trigger ferroptosis. This compound exhibits an IC50 of 0.386 μM against the non-small cell lung cancer (NSCLC) cell line H1975 and significantly suppresses the colony formation and migration abilities of H1975 and A549 cells, while also inducing apoptosis. Additionally, EGFR-IN-150 prominently reduces tumor growth in H1975 tumor-bearing mouse CDX models. It holds promise for research related to non-small cell lung cancer.

PRMT5-MTA-IN-3 (Compound P2A) is an orally active and selective inhibitor of protein arginine methyltransferase 5 (PRMT5). It inhibits the proliferation of MTAP-deficient colorectal cancer HCT-116 cell line with an IC50 value of 5 nM. PRMT5-MTA-IN-3 holds potential for research in cancers, particularly in MTAP-deficient tumors such as colorectal cancer, non-small cell lung cancer, and pancreatic cancer.

KRASG12C IN-19 is a selective inhibitor of KRASG12C. It exhibits potent antiproliferative activity against the KRASG12C-mutant non-small cell lung cancer (NSCLC) cell line H358, with an IC50 of 7.6 nM, and effectively inhibits downstream ERK phosphorylation (IC50= 24.06 nM). It shows no significant inhibitory activity on KRASG12V and KRASG12D mutant cancer cells (PANC 1, Panc 03.27, AsPC 1, and GP2d cells) with IC50 values greater than 10,000 nM. KRASG12C IN-19 rapidly forms a covalent bond with KRASG12V-GDP, leading to dose-dependent inhibition of the downstream KRAS pathway. This compound is suitable for research on KRASG12C-driven cancers, including non-small cell lung cancer, pancreatic cancer, and colorectal cancer.

KARS-IN-1 (152) is an AKR1C3-dependent KARS inhibitor with an AC50 of 9.1 nM for human KARS. It exhibits antiproliferative activity in both H460 (NRF2 pathway-mutant cell line with high AKR1C3 expression) and Hara (NRF2 pathway wild-type cell line with low AKR1C3 expression), with AC50 values of 21 nM and 16 nM, respectively. KARS-IN-1 is applicable in non-small cell lung cancer (NSCLC) research.

EGFR-IN-59 is a potent and selective EGFR inhibitor. It downregulates PI3K/AKT/mTOR signaling by blocking receptor autophosphorylation, exhibiting significant anti-proliferative activity in A431 and NSCLC cells.

RKS262 is a specific cyclin/CDK inhibitor. RKS262 was identified by structural optimization of Nifurtimox which is currently undergoing phase II clinical trials to treat high-risk neuroblastoma. In a NCI(60) cell-line assay RKS262 exhibited significant cytotoxicity in ovarian cancer cells and a variety of other cell lines exceeding effects of commercial drugs such as cisplatin, 5-FU, cyclophosphamide or sapacitabine. Various leukemia cell-lines were most sensitive (GI(50): ~ 10 nM) while several non-small cell lung cancer cell lines and few cell lines from other tissues were relatively resistant (GI(50) > 1 µM) to RKS262 treatment.

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.

EGFRkinase inhibitor 7 (compound 18i) is an EGFR inhibitor with an IC50 of 42.3 nM, exhibiting anticancer properties. This compound demonstrates significant in vitro cytotoxicity and capacity to induce apoptosis. Furthermore, EGFRkinase inhibitor 7 displays anti-proliferative activity against human colon cancer cell line HCT116 and human non-small cell lung cancer cell line A549, with IC50 values of 4.82 µM and 1.43 µM, respectively.

Agatharesinol acetonide shows anticancer activity towards the A549 non-small-cell lung-cancer cell line (IC50 = 27.1 microM).