NSCLC cells

PRLX-93936 HCL is an analog of erastin and demonstrated synergistic effects against non-small cell lung cancer (NSCLC) cells with cisplatin.

iMDK quarterhydrate is a potent PI3K inhibitor that inhibits the growth factor MDK (also known as midkine or MK). iMDK quarterhydrate synergistically inhibits non-small cell lung cancer (NSCLC) with MEK inhibitors without harming normal cells and mice.

Afatinib Dimaleate (BIBW 2992MA2) is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity.

NT157 is a small molecule tyrphostin targeting IRS protein and has the potential to inhibit IGF-1R and STAT3 signaling pathways in TME cancer cells and stromal cells, resulting in decreased cancer cell survival.

RMC5127 is an oral and mutation-selective inhibitor of RASG12V (ON) that inhibits the GTP-bound (ON) form of RAS G12V through the formation of a high-affinity triplex with central nervous system (CNS) permeability and brain permeability. RMC5127 inhibits RAS pathway activity in vitro in KRAS G12V mutant human cancer cells and cellular proliferation, and antitumor activity in preclinical intracranial xenograft models and subcutaneous CDX and PDX models of KRAS G12V mutant NSCLC, PDAC and CRC.

Peruvoside (Encordin) is a natural cardiac glycoside that inhibits Na+ K+-ATPase to increase myocardial contractility; causes cell cycle arrest in leukemia stem cells at the G₂ M phase, and; inhibits NSCLC cell growth as a Src inhibitor; and induces apoptosis in cancer cells through MAPK Wnt β-catenin and PI3K AKT mTOR .

ES-072, a selective inhibitor targeting the EGFR mutant (EGFR-T790M), is administered orally. By hindering EGFR-T790M activity, it activates GSK3α, which subsequently leads to the phosphorylation of PD-L1 at Ser279 and Ser283. This phosphorylation facilitates the recruitment of the E3 ubiquitin ligase ARIH1, resulting in the ubiquitination and proteasomal degradation of PD-L1. Such a process not only curtails the growth of cancer cells but also amplifies the anti-tumor immune response by diminishing PD-L1 levels. ES-072 has shown efficacy in impeding the proliferation of non-small cell lung cancer (NSCLC) cells.

NHTD, a KRAS-PDEδ inhibitor, exerts its function by targeting the isoprenyl binding pocket of PDEδ, which alters the cellular localization of KRAS. This modification restricts the proliferation of cancer cells with KRAS mutations and induces cell apoptosis (Apoptosis). NHTD is utilized in the study of KRAS-driven non-small cell lung cancer (NSCLC).

And1 degrader 1 (Compound A15) is a degrader of acidic nucleoplasmic DNA-binding protein 1 (And1) that notably induces degradation of And1 in NSCLC cells. When combined with Olaparib (1 μM), And1 degrader 1 at a concentration of 5 μM effectively inhibits proliferation in A549 and H460 cells. This compound is applicable in cancer research studies.

Top HDAC-IN-3 (Compound 31) is a dual inhibitor of Topoisomerase and HDAC with oral activity. It induces DNA damage by elevating reactive oxygen species (ROS) levels, consequently inhibiting the clonal formation and migration of cancer cells, and triggering apoptosis (Apoptosis) and cell cycle arrest. Top HDAC-IN-3 demonstrates a significant antitumor effect in NSCLC models, exhibiting a tumor growth inhibition (TGI = 77.5%, 100 mg kg) superior to that of the HDAC inhibitor SAHA and the combination of SAHA with the topoisomerase inhibitor Irinotecan.

NA-17 is a naphthalimide compound with antitumor activity and exhibits lower toxicity to normal cells such as HL-7702 and WI-38. It demonstrates p53-dependent inhibition selectivity in various NSCLC cells, inducing the accumulation of active p53 in the mitochondria and nuclei of these cells. NA-17 causes cell cycle arrest in the G1 phase and promotes apoptosis and cell death.

EGFR-IN-139 (compound PD 18) is an EGFR inhibitor with IC50 values of 12.88 nM (wild type), 10.84 nM (L858R T790M), and 42.68 nM (L858R T790M C797S). It demonstrates significant anticancer activity against the A549 and H1975 cancer cell lines, which express high levels of EGFR. EGFR-IN-139 exhibits strong selectivity for cancer cells and can be utilized in research on non-small cell lung cancer (NSCLC).

EGFRT790M L858R-IN-9 (Compound 8) is an inhibitor targeting the EGFR-L858R T790M mutations. It effectively inhibits the phosphorylation of the EGFR-L858R T790M mutant kinase, demonstrating an IC50 value of 0.0064 µM. Additionally, EGFRT790M L858R-IN-9 can suppress the proliferation of non-small cell lung cancer (NSCLC) cells, making it useful for cancer research.

PROTACROR1degrader-1 (Compound 11d) serves as a PROTAC degrader targeting the pseudokinase ROR1, with the capability of degrading ROR1 in NSCLC cells at a DC50 of 40-80 nM. It induces PARP cleavage and apoptosis in NCI-H23 cells. [Pink: ligand for target protein ROR1 ligand-1; Black: linker; Blue: ligand for VHL E3 ligase (S,R,S)-AHPC]

CDK9-IN-36 (Compound T7) is a potent, selective, and metabolically stable CDK9 inhibitor with an IC50 value of 1.2 nM. It effectively suppresses the proliferation of Osimertinib-resistant NSCLC cells by downregulating Mcl-1, reducing colony formation, and inducing apoptosis. Additionally, CDK9-IN-36 exhibits antitumor activity in xenograft models.

RET-IN-29 (Compound 8W) is a selective RET kinase inhibitor. It demonstrates inhibitory effects on BaF3 cells with the CCDC6-RETV804M mutation, with an IC50 of 0.715 μM. RET-IN-29 shows potential for research in non-small cell lung cancer (NSCLC).

Dornidazole (PR-000350, PR-350, RP-343, PR-69) is an effective radiosensitizer for hypoxic cells with the potential for the treatment of non-small cell lung cancer (NSCLC) and pancreatic cancer.

SW044248 is a noncanonical Top1 inhibitor. It has selective toxicity for NSCLC cells.

Ingenol 3,20-dibenzoate is a powerful activator of protein kinase C (PKC) isoforms that effectively induces the translocation of nPKC-delta, -epsilon, and -theta, as well as PKC-mu, from the cytosolic fraction to the particulate fraction. Through de novo synthesis of macromolecules, it triggers apoptosis with characteristic morphology. Moreover, Ingenol 3,20-dibenzoate enhances IFN-γ production and degranulation in NK cells, particularly when stimulated by NSCLC cells[1][2].

(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.

Ensartinib (X-396) is a potent and orally active dual ALK MET inhibitor for the treatment of ALK-positive non-small cell lung cancer (NSCLC).

CYH33, an orally active and highly selective PI3Kα inhibitor, demonstrates specificity with IC50 values of 5.9 nM for the α isoform, 598 nM for β, 78.7 nM for δ, and 225 nM for γ. It effectively inhibits Akt and ERK phosphorylation and induces substantial G1 phase arrest in breast cancer and non-small cell lung cancer (NSCLC) cells, showcasing potent activity against solid tumors.

CYH33 methanesulfonate is a highly selective and orally active inhibitor of PI3Kα, with IC50 values of 5.9 nM, 598 nM, 78.7 nM, and 225 nM against the α, β, δ, and γ isoforms, respectively. This compound effectively inhibits the phosphorylation of Akt and ERK, leading to a significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. Additionally, CYH33 methanesulfonate demonstrates potent activity against solid tumors.

iMDK quarterhydrate, a potent PI3K inhibitor, is effective in inhibiting the growth factor MDK (also known as midkine or MK) while demonstrating suppression of non-small cell lung cancer (NSCLC). In combination with a MEK inhibitor, iMDK quarterhydrate demonstrates cooperative inhibition of NSCLC without causing harm to normal cells and mice [1].