SM-7368 是一种NF-kB抑制剂，靶向抑制下游的MAPK p38。SM-7368 还抑制 TNF-α 诱导的MMP-9上调。SM-7368 可用于靶向 TNF-α 介导的肿瘤侵袭和转移的化疗研究。
| 生物活性 | SM-7368 is a potentNF-kBinhibitor that targets downstream ofMAPK p38activation[1]. SM-7368 inhibits TNF-α-inducedMMP-9upregulation. SM-7368 can be used for the research of chemotherapies targeting TNF-α-mediated tumor invasion and metastasis[2]. |
| IC50& Target[1][2] | NF-κB | MMP-9 | p38 MAP kinase |
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体外研究
(In Vitro) | SM-7368 (5 μM) targets downstream of MAPK p38 activation in the human colon derived crypt like HT-29 and Caco-2 epithelial cell lines[1].
SM-7368 inhibits TNF-α-induced MMP-9 upregulation in a concentration-dependent manner and shows maximal activity at 10 μM. SM-7368 inhibits TNF-α-induced MMP-9 mRNA transcript accumulation and protein expression. SM-7368 strongly inhibits TNF-α-induced NF-κB activity but not AP-1 activity. SM-7368 strongly inhibits the TNF-α-induced invasion of HT1080 human fibrosarcoma cell line[2].
SM-7368 (10-25 μM) greatly inhibits TNF-α (20 ng/mL)-induced MMP-9 upregulation. 10 μM of SM-7368 almost completely abrogates this upregulation[2].
Western Blot Analysis[2] | Cell Line: | HT1080 human fibrosarcoma cells | | Concentration: | 0, 1, 5, 10, 15, 20, and 25 μM | | Incubation Time: | 24 hours | | Result: | Greatly inhibited TNF-α (20 ng/mL)-induced MMP-9 upregulation in a concentration-dependent manner. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 83.33 mg/mL(253.52 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 3.0424 mL | 15.2119 mL | 30.4238 mL | | 5 mM | 0.6085 mL | 3.0424 mL | 6.0848 mL | | 10 mM | 0.3042 mL | 1.5212 mL | 3.0424 mL |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
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此方案可获得 ≥ 2.08 mg/mL (6.33 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 *以上所有助溶剂都可在本网站选购。
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