Cyclotriazadisulfonamide

Cyclotriazadisulfonamide (CADA) is a specific CD4 -targeted HIV entry inhibitors. Cyclotriazadisulfonamide (CADA) inhibits the co-translational translocation of human CD4 (huCD4) into the ER lumen in a signal peptide (SP)-dependent way. Cyclotriazadisulfonamide is also a Sec61 translocon inhibitor In Vitro Cyclotriazadisulfonamide (CADA) significantly decreases the amount of cell surface CD4 -the main receptor for HIV -without altering the expression of any other cellular receptor examined so far. Cyclotriazadisulfonamide (CADA) exhibits an EC 50 of 0.4 μg/mL for CD4 in MO-DC cells. Treatment of MO-DC with 10 μg/mL of CADA results in 83% downregulation of cell surface CD4, an effect that is similar to that observed for CADA treatment of CD4 + T cells. CADA prevents MT-4 cells from HIV-1 and SIV infection (EC 50 are 0.7 and 1.2 g/ml, respectively). Cyclotriazadisulfonamide is a Sec61 translocon inhibitor with a selective nature. A proteomics study on T-cells is performed and identified only five substrates (huCD4, SORT, CD137, DNAJC3, PTK7, ERLEC1) for Cyclotriazadisulfonamide, with IC 50 s of 0.2–2 µM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: MO-DCs. Concentration: 0.4 μg/mL. Incubation Time: 24 h. Result: A 50% reduction in CD4 expression was obtained. IC50& Target:HIV-1

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