NSC 74859 (Synonyms: S3I-201;NSC74859;NSC-74859;S3I 201) |
| Catalog No.GC14653 |
NSC 74859(S3I-201)는 IC50이 86μM인 선택적 Stat3 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 501919-59-1
Sample solution is provided at 25 µL, 10mM.
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S3I-201 is a selective inhibitor of Stat3 with IC50 value of 86 μM [1].
In the in vitro Stat3 DNA-binding assay, S3I-201 showed potent inhibition of the Stat3 DNA-binding activity with an average IC50 of 86 μM. In the EMSA assay, S3I-201 selectively inhibited Stat3 DNA-binding activity over that of Stat1 and Stat5. It suppressed the complex formation of Stat1-Stat3 and Stat1-Stat1 with IC50 values of 160 and > 300 μM, respectively. Besides that, the unphosphorylated, inactive Stat3 monomer was found to restore the Stat3 DNA-binding activity inhibited by S3I-201, suggesting that the inhibition was independent on the activation status. In NIH 3T3/v-Src fibroblasts, S3I-201 inhibited the constitutive activation of Stat3 and reduced the pTyr-705 Stat3 levels. Moreover, S3I-201 was found to significantly induce apoptosis in cells with constitutively active Stat3 at concentration of 30–100 μM. S3I-201 also reduced the expression of cyclin D1, Bcl-xL and surviving in these cells [1].
References:
[1] Siddiquee K, Zhang S, Guida W C, et al. Selective chemical probe inhibitor of Stat3, identified through structure-based virtual screening, induces antitumor activity. Proceedings of the National Academy of Sciences, 2007, 104(18): 7391-7396.
| Cell experiment: [1] | |
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Cell lines |
NIH 3T3/v-Src cells |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
|
Reaction Conditions |
100 μM, 24 hours |
|
Applications |
Viral Src transformed (NIH 3T3/v-Src) mouse fibroblasts stably expressing Stat3-YFP were transiently transfected with Flag-Stat3, treated with NSC-74859, and then subjected to pull-down assay and SDS/PAGE. Western blot analysis for FLAG of whole-cell lysates shows equal expression of the FLAG-ST3 protein in the lysates in the transiently transfected cells in both the control and NSC-74859-treated cells. Western blot analysis probing with anti-FLAG antibody showed no detectable level of FLAG-ST3 protein in the Stat3-YFP immunoprecipitates from NSC-74859-treated cells, suggesting the disruption by NSC-74859 of the complex formation between Stat3-YFP and FLAG-ST3 proteins. |
| Animal experiment: [1] | |
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Animal models |
Female athymic nude mice injected with MDA-MB-231 cells |
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Dosage form |
Intravenous injection, 5 mg/kg every 2 or 3 days for 2 weeks |
|
Applications |
Compared with control (vehicle-treated) tumors, which continued to grow, human breast tumors in mice that received NSC-74859 displayed strong growth inhibition. Continued evaluation of treated mice on termination of treatment showed no resumption of tumor growth, suggesting potentially a long-lasting effect of NSC-74859 on tumor growth. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Siddiquee K, Zhang S, Guida W C, et al. Selective chemical probe inhibitor of Stat3, identified through structure-based virtual screening, induces antitumor activity. Proceedings of the National Academy of Sciences, 2007, 104(18): 7391-7396. | |
| Cas No. | 501919-59-1 | SDF | |
| Synonyms | S3I-201;NSC74859;NSC-74859;S3I 201 | ||
| Chemical Name | 2-hydroxy-4-[[2-(4-methylphenyl)sulfonyloxyacetyl]amino]benzoic acid | ||
| Canonical SMILES | CC1=CC=C(C=C1)S(=O)(=O)OCC(=O)NC2=CC(=C(C=C2)C(=O)O)O | ||
| Formula | C16H15NO7S | M.Wt | 365.36 |
| Solubility | ≥ 18.25mg/mL in DMSO | Storage | Store at -20°C,unstable in solution, ready to use. |
| 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 | 2.737 mL | 13.6851 mL | 27.3703 mL |
| 5 mM | 0.5474 mL | 2.737 mL | 5.4741 mL |
| 10 mM | 0.2737 mL | 1.3685 mL | 2.737 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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Calculation results:
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: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)
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