Home
Resources
Publications
The Ion Channel Activator CyPPA Inhibits Melanogenesis via the GSK3β/β-catenin Pathway

The Ion Channel Activator CyPPA Inhibits Melanogenesis via the GSK3β/β-catenin Pathway

Tai Kyung Noh, Seung Hyun Bang, Ye Jin Lee, Hong Il Cho, Mi Young Jung, Inki Kim, Chae Hun Leem, Sung Eun Chang

Chem Biol Interact. 2019 Feb 25;300:1-7.

PMID: 30597128

Abstract:

Research into materials that inhibit melanogenesis in skin has gained interest. Screening for such compounds in B16F10 cells revealed that cyclohexyl-[2-(3,5-dimethyl-pyrazol-1-yl)-6-methyl-pyrimidin-4-yl]-amine (CyPPA), a positive modulator of small-conductance Ca2+-activated K+ channels, is a strong inhibitor of melanogenesis. We investigated the anti-melanogenic activity of CyPPA and the molecular mechanism by which CyPPA reduced melanin production in normal human melanocytes (NHM). CyPPA treatment resulted in a significant concentration-dependent reduction in melanin content without significant cytotoxicity; treatment likewise resulted in a significant time-dependent reduction in tyrosinase (TYR) activity. Treatment with CyPPA also decreased transcription of melanogenesis-related genes, including the gene encoding microphthalmia-associated transcription factor (MITF). In addition, visual evaluation of the MelanoDerm™ human skin model revealed significantly lower melanin content in the CyPPA-treated condition than in the untreated control. CyPPA was determined to modulate glycogen synthase kinase-3β (GSK3β) activity, thereby leading to a decrease in β-catenin/MITF expression. Thus, CyPPA acts as a melanogenesis inhibitor by modulating the GSK3β/β-catenin/MITF pathway.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP73029739	CyPPA		73029-73-9	Price

As a specialist in analytical chemical Products, Alfa Chemistry offers consumers a wealth of raw materials and a full range of technologies and services.

QUICK LINKS

HEADQUARTERS

Tel:

Fax:

Email: