T37284 |
BI 6015 |
源叶(MedMol) | 98% |
- 产品描述: BI-6015 is a hepatocyte nuclear factor 4α (HNF4α) antagonist that can inhibit the expression of known HNF4α target genes. BI6015 represses insulin promoter activity through HNF4α antagonism. BI-6015 can be used for the research of cancer and diabetes
- 靶点: hepatocyte nuclear factor 4α (HNF4α)
- 体外研究: BI-6015 (1.25 -20 μM;24-72 h) 对人肝细胞癌 (HCC) 具有细胞毒性。 BI-6015 (2.5-10 μM;5-48 h) 在 HepG2 细胞中抑制 HNF4α 基因表达。 BI-6015 (5 μM;3 d) 在原代小鼠肝细胞中诱导肝脂肪变性 Cell Viability Assay Cell Line: Hep3B-Luc cells and primary hepatocytes Concentration: 1.25, 2.5, 5, 10, 20 μM Incubation Time: 24, 48, 72 hours Result: Was markedly toxic to Hep3B cells but spared primary hepatocytes.
- 体内研究: BI-6015 (10-30 mg/kg;每天腹腔注射一次,连续 5 天) 诱导小鼠 HNF4α 表达缺失和肝脂肪变性。 BI-6015 (10-30 mg/kg;ip 每天或每隔一天一次,持续 20-57 天) 在人肝细胞癌小鼠模型中诱导细胞凋亡
- 参考文献:
1. Kiselyuk A, et, al. HNF4α antagonists discovered by a high-throughput screen for modulators of the human insulin promoter. Chem Biol. 2012 Jul 27;19(7):806-18.
- 溶解性: Soluble in DMSO
- 保存条件: 2-8℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 3.018 ml 15.09 ml 30.18 ml 5 mM 0.604 ml 3.018 ml 6.036 ml 10 mM 0.302 ml 1.509 ml 3.018 ml 50 mM 0.06 ml 0.302 ml 0.604 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)