Cotransin

Cotransin is a Sec61 translocation inhibitor that acts in a signal-sequence-discriminatory manner to prevent the stable insertion of select nascent chains into the Sec61 translocation channel. Cotransin selectively inhibits the expression of VCAM-1 and p-selectin proteins by inhibiting their co-translational translocation across endoplasmic reticulum (ER) membranes (IC50=0.5-5 µM). Cotransin has potential for studying inflammation and immunity[1][2].

Signaling Pathways >> Others >> Others

Research Areas >> Inflammation/Immunology

Sec61[1][2].

Cotransin 通过抑制这些蛋白质跨内质网 (ER) 膜的共翻译易位来抑制 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 IC50 范围为 0.5-5 µM[1]。 Cotransin 抑制分泌蛋白和膜蛋白的子集的表达[2]。 Cotransin (1, 5 µM; 24 h) 在 COS-7 细胞中，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.

[1]. Eva Pauwels, et al. Inhibitors of the Sec61 Complex and Novel High Throughput Screening Strategies to Target the Protein Translocation Pathway. Int J Mol Sci, 2021, 22(21), 12007.

[2]. Garrison JL, Kunkel EJ, Hegde RS, Taunton J. A substrate-specific inhibitor of protein translocation into the endoplasmic reticulum. Nature. 2005 Jul 14;436(7048):285-9.