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。
| 生物活性 | NCGC00378430 is a potentSIX1/EYA2interaction inhibitor. NCGC00378430 partially reverses transcriptional and metabolic profiles mediated by SIX1 overexpression and reverses SIX1-induced TGF-β signaling and epithelial-mesenchymal transition (EMT). NCGC00378430 inhibits SIX1-mediated breastcancermetastasis in a mouse model[1].
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体外研究
(In Vitro) | NCGC00378430 is a potent SIX1/EYA2 interaction inhibitor with an IC50of 52 μM in the Alphascreen assay[1].
NCGC00378430 (20 μM; 3 days) blocks TGF-β induced activation of p-Smad3, upregulation of FN1, and downregulation of E-CAD in T47D cells[1].
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[1].
NCGC00378430 (10 or 20 μM) disrupts SIX1-EYA2 interaction in breast cancer cells (MCF7, T47D, MDA-MB-231 cells)[1].
NCGC00378430 (10 μM; for 3 days) partially reverses SIX1-mediated transcriptional and metabolic signatures in MCF7 breast tumor cells[1].
Western Blot Analysis[1] | Cell Line: | T47D cells | | Concentration: | 20 μM | | Incubation Time: | 3 days | | Result: | Blocked TGF-β induced activation of p-Smad3, upregulation of FN1, and downregulation of E-CAD. |
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体内研究
(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[1].
NCGC00378430 (20 mg/kg; IV) has a T1/2α of 0.25 hours[1].
| Animal Model: | 6-8 week old NSG mice with MCF7 tumor cells[1] | | Dosage: | 25 mg/kg | | Administration: | Local Injection to the site of tumor; every other day; from day 3 until the day 21 | | Result: | Dramatically decreased distant metastatic burden compared to vehicle treatment.
Had no growth inhibitory effect. |
| Animal Model: | Mice[1] | | Dosage: | 20 mg/kg (Pharmacokinetic Analysis) | | Administration: | IV | | Result: | Had a T1/2α of 0.25 hours, a CL of 6.19 L/hrokg, a Vssof 4.08 L/kg, a Cmaxof 6703 ng/mL and an AUC of 3234 ng/mLohr. |
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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 : 100 mg/mL(226.50 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.2650 mL | 11.3250 mL | 22.6501 mL | | 5 mM | 0.4530 mL | 2.2650 mL | 4.5300 mL | | 10 mM | 0.2265 mL | 1.1325 mL | 2.2650 mL |
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