RCM 1
规格
Cas Number | 339163-65-4 |
规格或纯度 | 10mM in DMSO |
包装 | 1ml |
产品信息
别名 | 2-[[[2-氧代-2-(2-噻吩基)乙基]硫代] -4,6-二-2-噻吩基-3-吡啶甲腈 |
品牌 | 阿拉丁 |
浓度 | 10mM in DMSO |
简短描述 | FOXM1抑制剂 |
英文简短描述 | FOXM1 inhibitor |
过滤标签 | Compound libraries |
储存温度 | -80℃储存 |
运输条件 | 超低温冰袋运输 |
生化和生理学机理 | 前叉箱M1(FOXM1)转录因子抑制剂(IC50 = 0.72μM)。抑制FOXM1靶基因的表达。在体外诱导FOXM1蛋白降解。在暴露于过敏原的小鼠中,降低气道阻力,增加肺顺应性并减少促炎细胞因子的产生。RCM-1 is a forkhead box M1 (FOXM1) inhibitor that blocks FOXM1 nuclear localization (IC50 = 720 nM using GFP-FOXM1-expressing U2OS cells) and causes FOXM1 degradation via ubiquitination induction (2.9- and 4.8-fold of basal level in A549 cells with 10 μM or 20 μM RCM-1, respectively) without affecting cellular YAP, FACT140, NF-κB, FOXA2, and FOXJ1 levels. RCM-1 intraperitoneal injection (1.7 mg/kg) in mice downregulates endogenous murine FOXM1 level as well as transgenic human FOXM1 GFP fusion level in vivo, effectively suppressing house dust mite-induced lung inflammation as well as goblet cell metaplasia and airway hyperresponsiveness in response to IL-13. |
描述 |
RCM-1 是一种 forkhead box M1 (FOXM1) 抑制剂,在 U2OS 细胞中的 EC50 为 0.72 μM。RCM-1 阻止了核定位并增加了 FOXM1 的蛋白酶体降解。RCM-1 可用于哮喘和其他慢性气道疾病的研究。 |