Hexachlorophene

Hexachlorophene (Hexachlorofen) is an effective anti-bacterial and antifungal agent. Hexachlorophene can cause lysis of protoplasts and leakage of intracellular contents in bacterial. Hexachlorophene is an inhibitor of SARS-CoV 3CL protease with an IC₅₀ value of 5 μM. Hexachlorophene is also a potent KCNQ1/KCNE1 potassium channel activator with an EC₅₀ value of 4.61 μM. Hexachlorophene inhibits Wnt/β-catenin signaling as well, and can be used in the research of arrhythmia, bacterial, cancers^[1][2][3][4]. IC50 & Target: EC50: 4.61 μM (KCNQ1/KCNE1)^[1];
IC50: 5 μM (SARS-CoV)^[4] In Vitro: Hexachlorophene (0.1-10 μM approximately) increases the current amplitude of KCNQ1/KCNE1 with an EC₅₀ value of 4.61 μM, and shortens the action potential^[1].
Hexachlorophene (10 μM) rescues the loss of function of the LQTs mutants caused by either impaired activation gating or PIP2 binding affinity in CHO cells^[1].
Hexachlorophene (0-50 μg/mL approximately, 30 min) has antibacterial activities against micrococcus sp., staphylococcus, staphylococcus epidermidis and streptococcus with IC₅₀ values of 0.83 μg/mL, 1.5 μg/mL, 1.75 μg/mL, 1.3 μg/mL, respectively^[2].
Hexachlorophene (20 μM, 15 h) inhibits Wnt/β-catenin signaling through the Siah-1-mediated β-catenin degradation in HEK293 and HCT116 cells^[3].
Hexachlorophene (0-10 μM, 48 h) inhibits the growth of HCT116 cells^[3].
Hexachlorophene is a competitive inhibitor of SARS-CoV 3CL with an IC₅₀ value of 5 μM, and can form hydrogen bonds with SARS-CoV 3CL with K_i value estimated to be 4 μM^[4]. In Vivo: Hexachlorophene (tail immersion for 5 minutes, 1.25% w/v, one day prior to cercarial exposure) has inhibitory activity against Schistosoma mansoni infections in mice (exposed to WRAIR,Puerto Rican strain)^[6].
Hexachlorophene has acute and subacute toxic effects with i.p. LD50 ranged between 21.8 mg/kg-40.0 mg/kg, and the oral LD50 varied from 57.6 to 87.0 mg/kg, respectively^[5].