sec61

Sec61-IN-2 (A3) is a protein secretion inhibitor.

Sec61-IN-1, a powerful Sec61 inhibitor, impedes the translocation of proteins across the endoplasmic reticulum membrane.

Sec61-IN-2 (A347) is a protein secretion inhibitor. This compound effectively interferes with the Sec61-mediated translocation mechanism, thereby inhibiting the movement of proteins across the endoplasmic reticulum membrane, which disrupts cellular functioning.

Sec61-IN-5 (Compound 16c), a Sec61 inhibitor, exhibits cytotoxicity in A549 cells with an IC50 of 0.27 nM and impedes Sec61-dependent secretory function with an IC50 of 0.08 nM [1].

Sec61-IN-4 (Compound 16b) is a potent inhibitor of Sec61, exhibiting an IC50 value of 0.04 nM in U87-MG cells [1].

FMP-401319-3 is a concentration-dependent inhibitor of CRF1R-pPL cotranslational translocation at the level of the Sec61 complex.

Apratoxin S4 (Apra S4), a potent inhibitor of Sec61, disrupts the cotranslational translocation of secretory proteins into the endoplasmic reticulum (ER), showcasing antiviral efficacy against select flaviviruses with IC 50 values spanning 0.46 nM to 170 nM. It also curtails retinal vascular cell activation by targeting various angiogenic pathways. This compound is valuable for investigating viral infections, angiogenic diseases, and cancers [1] [2].

Ipomoeassin F, a selective and potent inhibitor of endoplasmic reticulum (ER) protein translocation, targets the Sec61 complex's pore-forming subunit (Sec61α) at the ER membrane. It inhibits the ER membrane translocation of SARS-CoV-2 proteins and blocks the ER translocation of secretory and type I transmembrane proteins (TMPs), without affecting type III TMPs [1] [2] [3].

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].

CT-08 (CT8, Compound 3) is a macrolide Sec61 modulator that inhibits protein secretion in a signal sequence-dependent manner. It prevents the Sec61-mediated translocation of VCAMss-GLuc to the ER, resulting in the loss of luciferase activity. Additionally, CT-08 suppresses the expression of VCAM in transfected cells.