Cyclotriazadisulfonamide
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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.
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- Pureté: 98.45%
- CAS No.: 182316-44-5
- Formule: C31H39N3O4S2
- Masse moléculaire:581.79
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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HIV-1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | IC50 |
0.38 μM
Compound: CADA
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Inhibition of GFP-tagged Sortilin (unknown origin) expressed in HEK293T cells after 42 hrs by FACS analysis
Inhibition of GFP-tagged Sortilin (unknown origin) expressed in HEK293T cells after 42 hrs by FACS analysis
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[PMID: 32209293] |
| SUP-T1 | IC50 |
0.21 μM
Compound: CADA
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Inhibition of FITC-tagged human CD4 expressed in human SUP-T1 cells after 72 hrs by FACS analysis
Inhibition of FITC-tagged human CD4 expressed in human SUP-T1 cells after 72 hrs by FACS analysis
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[PMID: 32209293] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MO-DCs.
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Concentration:0.4 μg/mL.
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Incubation Time:24 h.
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Result:A 50% reduction in CD4 expression was obtained.
Chemical Information
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CAS No. 182316-44-5
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Appearance Solid
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Masse moléculaire 581.79
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Formule C31H39N3O4S2
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Color White to off-white
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SMILES
O=S(N1CC(CN(S(=O)(C2=CC=C(C)C=C2)=O)CCCN(CC3=CC=CC=C3)CCC1)=C)(C4=CC=C(C)C=C4)=O
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Synonyms
CADA
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 33.33 mg/mL (57.29 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7188 mL | 8.5942 mL | 17.1883 mL | 42.9708 mL |
| 5 mM | 0.3438 mL | 1.7188 mL | 3.4377 mL | 8.5942 mL | |
| 10 mM | 0.1719 mL | 0.8594 mL | 1.7188 mL | 4.2971 mL | |
| 15 mM | 0.1146 mL | 0.5729 mL | 1.1459 mL | 2.8647 mL | |
| 20 mM | 0.0859 mL | 0.4297 mL | 0.8594 mL | 2.1485 mL | |
| 25 mM | 0.0688 mL | 0.3438 mL | 0.6875 mL | 1.7188 mL | |
| 30 mM | 0.0573 mL | 0.2865 mL | 0.5729 mL | 1.4324 mL | |
| 40 mM | 0.0430 mL | 0.2149 mL | 0.4297 mL | 1.0743 mL | |
| 50 mM | 0.0344 mL | 0.1719 mL | 0.3438 mL | 0.8594 mL |
Cyclotriazadisulfonamide Related Classifications
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