Piperacetazine

Piperacetazine is an orally active dopamine receptor antagonist and phenothiazine antipsychotic. Piperacetazine can directly bind to the PAX3::FOXO1 fusion protein and inhibit its transcriptional activity. Piperacetazine also exhibits antitumor activity with an IC₅₀ of 7.627 μM against PANC-1 cells. Piperacetazine can be used for the research of diseases such as schizophrenia and pancreatic cancer and other tumors^[1][2][3]. In Vitro:Piperacetazine (10 μmol/L; 6 days) downregulates the protein expression of PAX3::FOXO1 target genes MYOD1, MYOG, and B7-H3 in RH30 cells without affecting the level of PAX3::FOXO1 itself^[1].
Piperacetazine (15 μmol/L; 19 days) inhibits the anchorage-independent growth of RH30 cells^[1]. In Vivo:Piperacetazine (20 mg/kg; intraperitoneal injection; 5 days per week; until tumor volume reaches 1.5 cm³) slows tumor growth in NOD-SCID mice inoculated with RH30 cells, but the difference is not statistically significant^[1].
Piperacetazine (0.005-0.025%; feed management; 1 year) is well-tolerated in rats^[2].
Piperacetazine (0.25-5.0 mg/kg; oral administration; 52 weeks) is well-tolerated in dogs^[2].