产品
编 号:F132965
分子式:C16H16F3N5
分子量:335.33
产品类型
结构图
CAS No: 1353867-91-0
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生物活性:
Longdaysin is a inhibitor of the Wnt/β-catenin signaling pathway, which exerts antitumor effect through blocking CK1δ/ε-dependent Wnt signaling. Longdaysin inhibits CK1α, CK1δ, CDK7, and ERK2 with IC50s of? 5.6 μM, 8.8 μM, 29 μM, and 52 μM, respectively.
体内研究:
Longdaysin (0-9 μM; 1 周) 可延长斑马鱼的昼夜节律。Longdaysin (5 mg/kg,腹腔注射,每 3 天一次,持续 3 周) 可抑制小鼠 MDA-MB-231 异种移植瘤的肿瘤生长。Animal Model:MDA-MB-231 xenografts
Dosage:5 mg/kg
Administration:i.p., every 3 days for 3 weeks
Result:Decreased tumor cell density and proliferation (indicated by Ki-67).Reduced the expression of active and total β-catenin, and decreased the expression of phosphorylated and total LRP6, phosphorylated DVL2, and active and total β-catenin.Reduced mRNA expression of the Wnt target genes including Axin2, DKK1, LEF1, and Survivin.
体外研究:
Longdaysin (0-9 μM; 1 周) 可延长 mPer2Luc 敲入小鼠的成年尾成纤维细胞、肺外植体和 SCN 外植体的昼夜节律。Longdaysin (0-25 μM; 1 周) 抑制乳腺癌 Hs578T 或 MDA-MB-231 细胞的集落形成、迁移、侵袭和球体形成。Longdaysin (0-50 μM; 24 小时) 通过抑制 HEK293T 细胞中的 CK1δ 和 CK1ε 来抑制 Wnt/β-catenin 信号传导。