NCGC00378430 |
| Katalog-Nr.GC62286 |
NCGC00378430 ist ein potenter SIX1/EYA2-Interaktionsinhibitor. NCGC00378430 kehrt teilweise Transkriptions- und Stoffwechselprofile um, die durch SIX1-Überexpression vermittelt werden, und kehrt die SIX1-induzierte TGF-β-SignalÜbertragung und den epithelial-mesenchymalen Übergang (EMT) um. NCGC00378430 hemmt die SIX1-vermittelte Brustkrebsmetastasierung in einem Mausmodell.
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Cas No.: 920650-00-6
Sample solution is provided at 25 µL, 10mM.
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NCGC00378430 is a potent SIX1/EYA2 interaction 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 breast cancer metastasis in a mouse model[1].
NCGC00378430 is a potent SIX1/EYA2 interaction inhibitor with an IC50 of 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].
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].
[1]. Hengbo Zhou, et al. Identification of a Small-Molecule Inhibitor That Disrupts the SIX1/EYA2 Complex, EMT, and Metastasis. Cancer Res. 2020 Jun 15;80(12):2689-2702.
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