Propafenone

Propafenone (SA-79), a sodium-channel blocker, acts an antiarrhythmic agent. Propafenone also has high affinity for the β receptor (IC₅₀=32 nM)^[1]. Propafenone blocks the transient outward current (Ito) and the sustained delayed rectifier K current (Isus) with IC₅₀ values of 4.9?μm and 8.6?μm, respectively^[2]. Propafenone suppresses esophageal cancer proliferation through inducing mitochondrial dysfunction and induce apoptosis^[3]. In Vitro: Propafenone (5-25 μM) inhibits esophageal squamous cell carcinoma (ESCC) cell proliferation^[3].
Propafenone causes mitochondrial dysfunction by a decreased mitochondrial membrane potential and reduced expression of Bcl-xL and Bcl-2^[3].
Propafenone (10 and 20 μm) treatment significantly down regulates the expression levels of the anti-apoptotic proteins Bcl-xL and Bcl-2 in ESCC cells. Propafenone also reduces expression of p-ERK^[3]. In Vivo: Propafenone (20 mg/kg; intraperitoneal injection every other day) markedly suppresses the tumor burden with a decrease of 69.2%^[3].
Propafenone also significantly inhibits tumor cell proliferation (mean index decreased from 56.3±6.7% in the DMSO-treated group to 20.7±5.1% in the 10 mg/kg propafenone-treated group and 11.3±4.0% in the 20 mg/kg propafenone-treated group)^[3].