产品
编 号:F146403
分子式:C13H19Cl2N3OS
分子量:336.28
产品类型
结构图
CAS No: 13860-66-7
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产品详情
生物活性:
N3PT (N3-pyridyl thiamine) is a potent and selective transketolase inhibitor. N3PT is pyrophosphorylated and then binds to transketolase with an Kd value of 22 nM (Apo-TK, transketolase lacking bound thiamine).
体内研究:
N3PT (compound 1) (100 mg/kg;iv;每天两次;2 周) 在 HCT-116 荷瘤裸鼠中显示出对转酮醇酶活性的抑制作用,但没有显著的抗肿瘤活性。Animal Model:HCT-116 tumor-bearing nude mice
Dosage:100 mg/kg
Administration:Intravenous injection; twice a day; 2 weeks
Result:Decreased the activity of transketolase with no apparent effect on tumor size.Indicated that there were alternative pathways to generate ribose for DNA synthesis that were operating in these tumor cell lines.
体外研究:
Transketolase 是肿瘤细胞磷酸戊糖途径中的关键酶。 N3PT (compound 1) 对人类的平均 EC50 值为 26 nM HCT-116 细胞中的转酮醇酶。 N3PT (1 ppm 或 5 ppm) 显著抑制硫胺素利用酶活性,而不减少含 NADPH 的葡萄糖 6-磷酸脱氢酶 (G6PD) 活动。