| Bioactivity | 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]. | ||||||||||||
| Target | EC50: 4.61 μM (KCNQ1/KCNE1); IC50: 5 μM (SARS-CoV) | ||||||||||||
| Invitro | 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 Ki value estimated to be 4 μM[4]. Western Blot Analysis[3] Cell Line: | ||||||||||||
| 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]. Animal Model: | ||||||||||||
| Name | Hexachlorophene | ||||||||||||
| CAS | 70-30-4 | ||||||||||||
| Formula | C13H6Cl6O2 | ||||||||||||
| Molar Mass | 406.90 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Zheng Y, et al. Hexachlorophene is a potent KCNQ1/KCNE1 potassium channel activator which rescues LQTs mutants. PLoS One. 2012;7(12):e51820. [2]. Lloyd WJ, et al. Cyclohexane triones, novel membrane-active antibacterial agents. Antimicrob Agents Chemother. 1988 Jun;32(6):814-8. [3]. Seoyoung Park, et al. Hexachlorophene inhibits Wnt/beta-catenin pathway by promoting Siah-mediated beta-catenin degradation. Mol Pharmacol. 2006 Sep;70(3):960-6. [4]. Yu-Chih Liu, et al. Screening of drugs by FRET analysis identifies inhibitors of SARS-CoV 3CL protease. Biochem Biophys Res Commun [5]. H S Nakaue, et al. Studies on the toxicity of hexachlorophene in the rat. Toxicol Appl Pharmacol. 1973 Feb;24(2):239-49. [6]. M M Grenan, et al. Hexachlorophene as a topically applied chemical for prophylaxis against Schistosoma mansoni infections in mice. Rev Inst Med Trop Sao Paulo. 1985 Jul-Aug;27(4):190-6. |
Hexachlorophene
CAS: 70-30-4 F: C13H6Cl6O2 W: 406.90
Hexachlorophene (Hexachlorofen) is an effective anti-bacterial and antifungal agent. Hexachlorophene can cause lysis of
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