Cotransin, a Sec61 translocation inhibitor, selectively prevents the stable insertion of certain nascent chains into the Sec61 translocation channel, exhibiting signal-sequence discrimination. This compound also inhibits the expression of VCAM-1 and p-selectin proteins by blocking their co-translational translocation across endoplasmic reticulum (ER) membranes (IC 50 =0.5-5 µM). Cotransin's role extends to potential applications in inflammation and immunity research [1] [2].

Cotransin通过抑制蛋白质在内质网(ER)膜的共翻译易位，抑制VCAM-1、P-选择素、血管紧张素原、β-内酰胺酶、CRF1、ETBR、AQP2、HER-3和TNF-α的表达，其IC 50范围为0.5-5 µM [1]。Cotransin抑制分泌蛋白和膜蛋白子集的表达 [2]。在COS-7细胞中，Cotransin (1, 5 µM; 24 h) 对VCAM1显示出选择性、有效和可逆的抑制作用 [2]。Cotransin阻止Sec61复合物的信号序列识别 [2]。Western Blot Analysis [2] Cell Line: COS-7 cells (transfected with a VCAM1 expression plasmid or not) Concentration: 1, 5 µM Incubation Time: 24 h Result: Showed selective, potent and reversible inhibition to VCAM1.