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Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
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| 规格： | 1 mg | 产品价格： | ￥860.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥1981.0 |
| 规格： | 10 mg | 产品价格： | ￥2984.0 |
| 规格： | 25 mg | 产品价格： | ￥5462.0 |
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NCGC00378430
CAS No. : 920650-00-6
MCE 国际站：NCGC00378430
产品活性：NCGC00378430 是一种有效的 SIX1/EYA2 相互作用抑制剂。NCGC00378430 部分逆转 SIX1 过表达介导的转录和代谢谱，并逆转 SIX1 诱导的 TGF-β 信号传导和上皮-间质转化 (EMT)。NCGC00378430 在小鼠模型中抑制 SIX1 介导的乳腺癌转移。
研究领域：Metabolic Enzyme/Protease
作用靶点：Phosphatase
In Vitro: NCGC00378430 is a potent SIX1/EYA2 interaction inhibitor with an IC50 of 52 μM in the Alphascreen assay.
?NCGC00378430 (20 μM; 3 days) blocks TGF-β induced activation of p-Smad3, upregulation of FN1, and downregulation of E-CAD in T47D cells.
?NCGC00378430 (10 μM; 3 days) reverses the Sine oculis homeobox homolog 1 (SIX1)-induced increase in p-SMAD3 and does not alter total E-CAD levels. NCGC00378430 restores membranous E-CAD in MCF7-SIX1 cells, along with inhibiting FN1 expression.
?NCGC00378430 (10 or 20 μM) disrupts SIX1-EYA2 interaction in breast cancer cells (MCF7, T47D, MDA-MB-231 cells).
?NCGC00378430 (10 μM; for 3 days) partially reverses SIX1-mediated transcriptional and metabolic signatures in MCF7 breast tumor cells.
In Vivo: NCGC00378430 (25 mg/kg; local injection to the site of tumor; every other day; from day 3 until the day 21) dramatically decreases distant metastatic burden compared to vehicle treatment.
?NCGC00378430 (20 mg/kg; IV) has a T1/2α of 0.25 hours.
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