Benproperine phosphate (Synonyms: ASA 158-5, BPP)

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].

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].

Benproperine phosphate (50, 100mg/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].

References:
[1]. Yae Jin Yoon, et al. Benproperine, an ARPC2 inhibitor, suppresses cancer cell migration and tumor metastasis. Biochem Pharmacol. 2019 May;163:46-59.