生物活性 | |||
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描述 | FOXM1 is a transcription factor from the Forkhead box (FOX) family that is critical for the differentiation of goblet cells from airway progenitor cells. RCM-1 is a FOXM1 inhibitor which inhibits goblet cell metaplasia and IL-13 signaling, and RCM-1 is used to treat patients with asthma and other chronic airway diseases. RCM-1 inhibited GFP-FOXM1 with an EC50 of 0.72 μM in U2OS cells. Furthermore, RCM-1 inhibited the expression of FOXM1 target genes Plk1 and Cdc25B, a functional readout of FOXM1 transcriptional activity. In addition to GFP-FOXM1, RCM-1 decreased the abundance of endogenous FOXM1 in primary human airway epithelial cells cultured on an air-liquid interface without altering that of other transcription factors. In vivo, RCM-1 treatment decreased the abundance of endogenous FOXM1 in wild-type BALB/c mice. RCM-1 protected lungs from HDM-induced airway hyperreactivity and preserved lung function in BALB/c mice. Moreover, RCM-1 decreased goblet cell metaplasia and airway resistance and improved lung function in IL-13-treated mice[2]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.36mL 0.47mL 0.24mL |
11.78mL 2.36mL 1.18mL |
23.55mL 4.71mL 2.36mL |
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