Kim, Su Yeon Hahn, Hoh-Gyu Nam, Kee Dal Park, Kyoung-Chan Yun, Hye-Young Baek, Kwang Jin Kwon, Nyoun Soo Kim, Dong-Seok 2024-01-20T16:33:38Z 2024-01-20T16:33:38Z 2021-09-04 2011-08 0022-3573 https://pubs.kist.re.kr/handle/201004/130149 Objectives We have investigated whether KHG25855 (2-cyclohexylamino-1,3-thiazole hydrochloride) affected melanogenesis in B16 mouse melanoma cells, and the mechanisms involved. Methods Melanin content and tyrosinase activity were measured using an ELISA reader after cells were treated with KHG25855. KHG25855-induced signalling pathways were examined using Western blot analysis. Key findings KHG25855 decreased melanin production in a dose-dependent fashion, but KHG25855 did not directly inhibit tyrosinase, the rate-limiting melanogenic enzyme. The expression of microphthalmia-associated transcription factor, tyrosinase, and the related signal transduction pathways were also investigated. The effects of KHG25855 on the extracellular signal-regulated kinase and cAMP response element binding protein signalling pathways were determined, and KHG25855 was shown to have no effect on these signalling pathways. The Wnt signalling pathway is also deeply involved in melanogenesis, and so glycogen synthase kinase 3 beta (GSK3 beta) phosphorylation was assessed after KHG25855 treatment; KHG25855 caused GSK3 beta phosphorylation (inactivation), but the level of beta-catenin was not changed by KHG25855. Furthermore, alpha-melanocyte stimulating hormone-induced tyrosinase expression was downregulated by KHG25855. Conclusions We propose that KHG25855 showed hypopigmentary activity through tyrosinase downregulation via GSK3 beta phosphorylation. English WILEY-BLACKWELL NORMAL HUMAN MELANOCYTES SKIN PIGMENTATION GENE-EXPRESSION CYCLIC-AMP MITF CAMP ACTIVATION PATHWAY AKT MICROPHTHALMIA A derivative of 2-aminothiazole inhibits melanogenesis in B16 mouse melanoma cells via glycogen synthase kinase 3 beta phosphorylation Article 10.1111/j.2042-7158.2011.01305.x 1 JOURNAL OF PHARMACY AND PHARMACOLOGY, v.63, no.8, pp.1031 - 1036 JOURNAL OF PHARMACY AND PHARMACOLOGY 63 8 1031 1036 scie scopus 000292263100006 2-s2.0-79959863109 Pharmacology & Pharmacy Pharmacology & Pharmacy Article NORMAL HUMAN MELANOCYTES SKIN PIGMENTATION GENE-EXPRESSION CYCLIC-AMP MITF CAMP ACTIVATION PATHWAY AKT MICROPHTHALMIA alpha-melanocyte stimulating hormone glycogen synthase kinase 3 beta KHG25855 melanogenesis tyrosinase