nci-h446

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

Doxycycline is an orally active tetracycline antibiotic with broad-spectrum inhibitory effects on matrix metalloproteinases (MMPs), possessing both antibacterial and antitumor activities, and is commonly used in inducible gene expression ON-OFF systems.

Doxycycline (hyclate) is an orally active tetracycline antibiotic with broad-spectrum inhibitory activity against matrix metalloproteinases (MMPs), possessing both antibacterial and antitumor properties, and is commonly used in inducible gene expression ON-OFF systems.

Talazoparib (LT-673) is a new-type PARP inhibitor (IC50: 0.58 nM), It similarly binds to PARP1/2 (Kis: 1.2/0.85 nM).

WEE1-IN-11 (Compound 13) serves as a potent CDK2 inhibitor with an IC50 of 2.0 nM. It exhibits inhibitory effects on several cell lines, including NCI-H446, A427, OVCAR3, C33A, and WiDr, with respective IC50 values of 93.9, 34.5, 86.7, 23.1, and 85 nM.

Topo I/II-IN-2 (Compound 3g) is an inhibitor of both Topo I and Topo II. It exhibits inhibitory activity against NCI-H446 and NCI-H1048 cells with IC50 values of 1.30 μM and 1.42 μM, respectively. Topo I/II-IN-2 induces mitochondrial apoptosis, disrupts mitochondrial function, and stimulates activity generation. Additionally, it inhibits the PI3K/Akt/mTOR pathway, effectively preventing the proliferation, invasion, and migration of small cell lung cancer (SCLC) cells in vitro.

PROTAC CDK9 degrader-11 (Compound C3) is an orally active PROTAC CDK9 degrader with a DC50 of 1.09 nM. This compound exhibits cytotoxicity in small cell lung cancer (SCLC) cells, with IC50 values in the nanomolar range. It induces cell cycle arrest at the G0/G1 phase and inhibits cell invasion in DMS114 and DMS53 cells. In addition, PROTAC CDK9 degrader-11 shows antitumor activity in an NCI-H446 xenograft mouse model. (Pink: ligand for target protein CDK9 ligand 3; Black: linker; Blue: ligand for E3 ligase Cereblon E3 ligase Ligand 56)

2E-3-F16 is an anticancer agent that exhibits tumor cell selectivity between NCI-H446 cancer cells and HBE cells. Additionally, 2E-3-F16 enhances the sensitivity of A549 cells to Cisplatin.

Dicycloplatin is an inducer of DNA damage. It activates doubly phosphorylated checkpoint kinase 2 (CHK2), breast cancer 1 (BRCA1), and triply phosphorylated p53 to induce DNA damage. Dicycloplatin can cause cell cycle arrest, inhibit proliferation, and trigger apoptosis in prostate cancer PC3 cells and lung cancer NCI/H446 cells. It is applicable for research in the field of cancer.

Rotundic acid (Rutundic acid), a natural compound, exhibit cytotoxic activities toward human hepatocellular carcinoma (HepG2), malignant melanoma (A375), SCLC (NCI-H446), breast cancer (MCF-7), and colon cancer (HT-29) cell lines.