Cyclotriazadisulfonamide (CADA) 是一个特异性的 CD4 靶向的 HIV 进入抑制剂。Cyclotriazadisulfonamide (CADA) 以信号肽依赖的途径抑制 CD4 进入 内质网腔进行共翻译转位。Cyclotriazadisulfonamide 也是一种 Sec61 转位子抑制剂。

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.

Solid

HIV-1

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 EC50 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 (EC50 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 IC50s of 0.2–2 μM.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Kurt Vermeire, et al. CADA, a potential anti-HIV microbicide that specifically targets the cellular CD4 receptor. Curr HIV Res. 2008 May;6(3):246-56.
[2]. Victor Van Puyenbroeck, et al. Preprotein signature for full susceptibility to the co-translational translocation inhibitor cyclotriazadisulfonamide. Traffic. 2020 Feb;21(2):250-264.

In Vitro: DMSO : 33.33 mg/mL (57.29 mM; Need ultrasonic and warming)配制储备液