A Ceramide-Trafficking Protein (CERT) Inhibitor

HPA-12 (1) is a ceramide (Cer) -trafficking inhibitor that was first discovered and synthesized by Hanada and Kobayashi et al.^1,2) Ceramide is synthesized in the endoplasmic reticulum (ER) and is transported to the Golgi apparatus,^3,4) where it is converted to sphingomyelin, by means of the ceramide transport protein (CERT).⁵⁾ 1 inhibits the CERT, and has been used as a CERT inhibitor in various biological science studies.⁶⁾ For example, 1 possesses antiviral and antibacterial properties against the growth of hepatitis C virus (HCV) and the obligate intracellular bacteria Chlamydiae in cultured human cells.^6a,d,e) In addition, the CERT inhibition results in resensitization of cancer cells to chemotherapeutic agents such as paclitaxel.^6b) Therefore, the inhibition of CERT may represent medical strategies, such as anti-infective and anticancer chemotherapy.

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