NS3694 (Synonyms: Apoptosis Inhibitor II) |
| Catalog No.GC12639 |
디아릴우레아 화합물인 NS3694는 세포자멸사 억제제입니다. NS3694는 apoptosome 형성과 caspase 활성화를 억제합니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 426834-38-0
Sample solution is provided at 25 µL, 10mM.
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IC50: approximately 50 μM for cytochrome c-induced caspase activation in HeLa cell cytosolic extracts
NS3694 inhibits apoptosome formation and caspase activation.
The release of mitochondrial proapoptotic proteins into the cytosol is a critical event in apoptosis signaling, resulting in the activation of caspases. Once in the cytosol, cytochrome c triggers the formation of a caspase-activating protein complex called the apoptosome, while Smac/Diablo and Omi/htra2 antagonize the caspase inhibitory effect.
In vitro: Previous study found that NS3694, and its two analogs (NS1764 and NS1784) were well-tolerated by MCF-7S1 breast cancer cells at concentrations up to 100, 50, and 25 μM, respectively. Moreove, all three compounds could not inhibit recombinant caspase 9 and caspase 3 at concentrations ranging from 25 to 100 μM. In addition, NS3694 was able to inhibit the co-immunoprecipitation of caspase 9 and Apaf-1 from HeLa cell cytosol stimulated by cytochrome c and dATP. NS3694 could also inhibit the formation of the active 700-kDa apoptosome complex, but had no effect on TNF-induced caspase-independent death of WEHI-S cells. NS3694 did not inhibit FasL-induced caspase activation or death in type I cells neither [1].
In vivo: Up to now, there is no animal in vivo study reported.
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Lademann, U. ,Cain, K.,Gyrd-Hansen, M., et al. Diarylurea compounds inhibit caspase activation by preventing the formation of the active 700-kilodalton apoptosome complex. Mol.Cell Biol. 23(21), 7829-7837 (2003).
| Cas No. | 426834-38-0 | SDF | |
| Synonyms | Apoptosis Inhibitor II | ||
| Chemical Name | 4-chloro-2-[[[[3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-benzoic acid | ||
| Canonical SMILES | ClC1=CC=C(C(O)=O)C(NC(NC2=CC=CC(C(F)(F)F)=C2)=O)=C1 | ||
| Formula | C15H10ClF3N2O3 | M.Wt | 358.7 |
| Solubility | ≤14mg/ml in ethanol;20mg/ml in DMSO;25mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7878 mL | 13.9392 mL | 27.8784 mL |
| 5 mM | 0.5576 mL | 2.7878 mL | 5.5757 mL |
| 10 mM | 0.2788 mL | 1.3939 mL | 2.7878 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 26 reference(s) in Google Scholar.)
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