Apoptosis Inducers

Difopein, dimeric version of R18 peptide that binds to 14.3.3 proteins with high affinity.

4-Oxo-4-HPR is an inhibitor of tubulin polymerization, inducing marked G2-M cell cycle arrest and apoptosis in fenretinide-sensitive and fenretinide-resistant cell lines. It is also a fenretinide metabolite.

Anticancer agent 299 is a cell-cycle inhibitor that functions as a senescence and apoptosis inducer, exhibiting significant antiproliferative effects on cancer cells. This compound demonstrates selective cytotoxicity against cancerous cells with minimal impact on non-tumoral chondrocyte cells at therapeutic concentrations. Anticancer agent 299 is particularly useful for research related to ER+/HER2− breast cancer and BRAF-mutant melanoma.

Homoharringtonine is a cephalotaxine alkaloid which inhibits the formation of diphenylalanine and acetylphenylalanyl-puromycin in liver ribosomes.

Kumatakenin is a potent apoptosis inducer and autophagy inhibitor that targets ATG5 with a Kd value of 2.94 μM. It effectively enhances the activity of caspases 3, 8, and 9, leading to caspase-dependent apoptosis in ovarian cancer cells while modulating chemokines and pro-oncogenic factors. Kumatakenin also reduces M2 macrophage polarization, inhibits tumor progression in esophageal cancer by targeting FASN, and interacts with Eno3 to mitigate ferroptosis and alleviate intestinal inflammation. This compound is valuable for studies in ovarian cancer, esophageal cancer, depression, and colitis research.

N-Desmethyldauricine is an inhibitor of NF-κB p65 with significant apoptotic effects. It effectively reduces p65 protein expression, induces apoptosis, and arrests the cell cycle at the G0/G1 phase. Additionally, N-Desmethyldauricine attenuates intercellular adhesion and inhibits the growth of 3D spheroids derived from triple-negative breast cancer. This compound is useful for research involving triple-negative breast cancer dynamics and therapeutic strategies.