NSC 74859
(Synonyms: S3I-201;NSC74859;NSC-74859;S3I 201,) 目录号 : GC14653
A STAT3 inhibitor
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. |
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Reaction Conditions |
100 μM, 24 hours |
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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 |
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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. |
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| Cas No. | 501919-59-1 | SDF | |
| 别名 | S3I-201;NSC74859;NSC-74859;S3I 201, | ||
| 化学名 | 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 | ||
| 分子式 | C16H15NO7S | 分子量 | 365.36 |
| 溶解度 | ≥ 18.25mg/mL in DMSO | 储存条件 | Store at -20°C,unstable in solution, ready to use. |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet