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PU 02,5-HT3受体的负变构调节剂

    
10mM in DMSO

6-[(1-NaphthalenylMethyl)thio]-9H-purine

源叶(MedMol)
V53376 一键复制产品信息
313984-77-9
C16H12N4S
292.36
PU-02
货号 规格 价格 上海 北京 珠海 重庆 武汉 购买数量
V53376-1ml
10mM in DMSO

¥630.00

货期:3-5天 - - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品
产品描述: PU02, a derivative of 6-MP (HY-13677), is a negative allosteric modulator (NAM) of 5-HT3 receptor, with IC50 values of 0.36 and 0.73 μM in HEK293 cells transfected with human 5-HT3A and 5-HT3AB receptors respectively
靶点: 5-HT3A Receptor:0.36 μM (IC50);5-HT 3 AB:0.73 μM (IC50);Apoptosis;5-HTReceptor
体外研究: PU02 (NMMP) (0-200 μM) leads to a steady decrease in cell viability of HepG2 cells (IC50=48.585 μM). PU02 (NMMP) shows less toxicity on L02 cells than did 6-MP after 48 h of treatment[2].
PU02 (NMMP) at 6.25 or 25 μM exhibits inhibitory effects on the viability of the tested cell lines, including SMMC-7721, MDA-MB-231, RKO and HCT-8 cells.

PU02 (NMMP) induces cell cycle arrest at the G2/M phase. PU02 (NMMP) downregulats the expression of cyclin B1/D1 and CDK4 in a time-dependent manner in HepG2 cells,but the expression of cyclin E is not affected.

PU02 (NMMP)-treated cells exhibits a significant increase in caspase-3 cleavage, suggesting enhanced apoptotic activity.
参考文献: 1. Sarah M Trattnig, et al. Discovery of a novel allosteric modulator of 5-HT3 receptors: inhibition and potentiation of Cys-loop receptor signaling through a conserved transmembrane intersubunit site. J Biol Chem. 2012 Jul 20;287(30):25241-54.

2. Xiao-Guang Yang, et al. 6-[(1-naphthylmethyl)sulfanyl]-9H-purine induces G2/M phase arrest and apoptosis in human hepatocellular carcinoma HepG2 cells. Eur J Pharmacol. 2012 Nov 15;695(1-3):27-33.
溶解性: Soluble  in  DMSO
保存条件: -80℃(运输条件:冰袋低温运输)
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 3.42 ml 17.102 ml 34.204 ml
5 mM 0.684 ml 3.42 ml 6.841 ml
10 mM 0.342 ml 1.71 ml 3.42 ml
50 mM 0.068 ml 0.342 ml 0.684 ml
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参考文献

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