| Bioactivity | 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[1][2][3]. | ||||||||||||
| Invitro | 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[1].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[1].CADA prevents MT-4 cells from HIV-1 and SIV infection (EC50 are 0.7 and 1.2 g/ml, respectively)[1].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[3]. Western Blot Analysis[1] Cell Line: | ||||||||||||
| Name | Cyclotriazadisulfonamide | ||||||||||||
| CAS | 182316-44-5 | ||||||||||||
| Formula | C31H39N3O4S2 | ||||||||||||
| Molar Mass | 581.79 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [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. [3]. Pauwels E, et al. Inhibitors of the Sec61 Complex and Novel High Throughput Screening Strategies to Target the Protein Translocation Pathway. Int J Mol Sci. 2021 Nov 5;22(21):12007. |
Cyclotriazadisulfonamide
CAS: 182316-44-5 F: C31H39N3O4S2 W: 581.79
Cyclotriazadisulfonamide (CADA) is a specific CD4-targeted HIV entry inhibitors. Cyclotriazadisulfonamide (CADA) inhibit
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