sms2-in-2

SMS2-IN-2 (SMS2 inhibitors) 是一种具有高度选择性、口服具有活力的鞘磷脂合成酶 2 抑制剂，能够作用于 SMS2 (IC50:100 nM)和 SMS1 (IC50:56 nM)。它可减轻慢性炎症反应。

SMS2-IN-1 是一种有效且具有高选择性的鞘磷脂合成酶 2 (SMS2) 抑制剂， IC50 为 6.5 nM，Kd 为 37 nM。SMS2-IN-1 对 SMS2 的选择性比 SMS1 (IC50 为 1000 nM) 多 150 倍。

Ceramide phosphoethanolamine (CPE) is an analog of sphingomyelin that contains ethanolamine rather than choline as the head group. It is the principal membrane phospholipid in invertebrates such as Drosophila, which lacks sphingomyelin. It is only produced in small amounts in mammalian cells, accounting for approximately 0.02 mol% of total phospholipids in mouse testis and brain. In Drosophila, CPE is biosynthesized by CPE synthase from ceramide and cytidine diphosphate-ethanolamine in the Golgi lumen. In mammals, it is biosynthesized by sphingomyelin synthase 2 (SMS2) in the plasma membrane and by sphingomyelin synthase-related protein (SMSr) in the endoplasmic reticulum (ER). In Drosophila, CPE has a role in glial ensheathment of axons. Disrupting CPE synthesis by depleting SMSr in vitro in mammalian cells leads to an accumulation of ER ceramides, which are then mislocalized to the mitochondria, inducing apoptosis. However, ceramide levels are not altered in transgenic mice lacking SMSr catalytic activity. CPEs (bovine) is a mixture of CPEs with variable N-acyl chain lengths.