Benproperine (phosphate)

Benproperine phosphate is an orally active, potent actin-related protein 2/3 complex subunit 2 (ARPC2) inhibitor. Benproperine phosphate attenuates the actin polymerization rate of action polymerization nucleation by impairing Arp2/3 function. Benproperine phosphate has the potential for a cough suppressant and suppresses cancer cell migration and tumor metastasis^[1]. In Vitro: Benproperine phosphate (20-120 μM; for 24 hours) inhibits cell viability in a dose-dependent manner^[1].
Benproperine phosphate (10 μM; for 24 hours) significantly inhibits the migration of various types of cancer cells and inhibits the migration and invasion of DLD-1, AsPC-1 cells with IC₅₀ values of 1-2 μM. Benproperine phosphate (10 μM; for 24 hours) does not affect cortactin-rich lamellipodium in MCF-10A cells^[1].
In Vivo: Benproperine phosphate (50, 100 mg/kg; oral gavage; 5 days per week for 4 weeks) inhibits primary pancreatic tumor growth^[1].
Benproperine phosphate shows a marked decrease in the lung metastasis of AsPC-1 cells (56.1% inhibition) in mouse. Benproperine phosphate significantly suppressed the liver metastasis of HCT-116 cells by 78.9% and DLD-1 cells by 78.2%^[1].