FPDT is an anti-glioblastoma agent and shows anti-glioblastoma activity by AKT pathway.

FPDT (2-(4-fluorophenyloamino)-5-(2,4-dihydroxyphenyl)-1,3,4-thiadiazole) is an anti-glioblastoma agent. FPDT displays cytotoxic with IC50 values of 44-68 μM for GBM cells and >100 μM for human astrocytes HA. Besides, Anti-glioblastoma activity of FPDT is linked to downregulation of the AKT pathway. FPDT (0-100 µM; 48 h) shows anti-proliferative activity with IC50 values of 53.53, 44.98, 55.20, 56.37, 67.73, >100...

CQ211 is a Potent and Selective RIOK2 Inhibitor

RIOK2 is a typical kinase implicated in multiple human cancers. The right open reading frame (RIO) kinases belong to the atypical kinases family. RIO kinases contain a C-terminal RIO domain that is structurally homologous to typical protein kinases. However, RIOKs lack the key motifs which can convert the enzyme from...

Lapatinib is a Potent Inhibitor of the ErbB-2 and EGFR Tyrosine Kinase Domains

Growth factors and their transmembrane receptor tyrosine kinase play important roles in cell proliferation, survival, migration, and differentiation. Additionally, Epidermal growth factor (EGF)-like proteins stimulates cells to divide by activating members of the EGF receptor (EGFR) family. Many types of human tumor cells growth and development are related to the...

Rebeccamycin, an Antitumor Antibiotic, Inhibits DNA Topoisomerase I

Rebeccamycin, a yellow crystalline product, is isolated from the mycelium. It has activity against P388 leukemia, L1210 leukemia, and B16 melanoma implanted in mice. Rebeccamycin is also an antitumor antibiotic produced by the actinomycete Saccharotrix aerocolonigenes with activity against several human tumor cell lines, including A549 (lung adenocarcinoma), HCT-116...

DS17701585 is a Highly Selective, Orally Active EP300 and CBP Inhibitor

DS17701585 (Compound 11) is a highly selective, orally active EP300 and CBP inhibitor with IC50 values of 0.15, 0.040, 0.45 and 0.70 µM against CBP, EP300, H3K27 and SOX2. Besides, DS17701585 has the potential for the research of cancer. EP300 and its paralog CBP play an important role in post-translational modification as...

Actinomycin D Inhibits DNA Repair and Induces Autophagy

Actinomycin D is isolated from Streptomyces species, containing a phenoxazine chromophore and two cyclic pentapeptide lactone rings. Besides, Actinomycin D can inhibit DNA repair, DNA-directed RNA synthesis, or DNA synthesis via binding to double-stranded DNA and the phenoxazine chromophore inserting DNA bases. Therefore, it acts as a DNA intercalator and...