您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > YM-201636
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
YM-201636
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
YM-201636图片
CAS NO:371942-69-7
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
YM201636 是是一种特异性 PIKfyve 抑制剂,IC50值为 33 nM,对 p110α的IC50为 3.3 μM。它还可抑制逆转录病毒复制。

产品描述

YM201636 (IC50=33 nM), a specific PIKfyve inhibitor, is less effective to p110α and insensitive to Fabl, which is yeast orthologue.

体内活性

在血清饥饿处理的NIH3T3细胞中, YM201636(0.8 μM)明显降低PtdIns(3,5)P2产量,降低达 80%。在3T3L1脂肪细胞中,YM-201636(IC50=54 nM)抑制2-脱氧葡萄糖吸收, 按160 nM剂量处理时,则能够完全抑制2-脱氧葡萄糖吸收。在MDCK细胞中,YM201636细胞间隙连接蛋白Claudin-1和Claudin-2的连续再循环,导致细胞内累积,也延迟上皮屏障的形成。

激酶实验

Following 3T3L1 adipocyte serum-starvation and insulin stimulation, cell lysates containing protease inhibitors are clarified and then subjected to immunoprecipitation with anti-PIKfyve antibodies. Washed beads are mixed with 100 μM PtdIns and preincubated for 15 min with YM-201636 (100 nM) or vehicle in the assay buffer (50 mM Tris-HCl, pH 7.5, 1 mM EGTA and 10 mM MgCl2). The kinase assay (50 μL final volume) is carried out for 15 min at 37 °C with 15 μM ATP and [γ-32P]ATP (30 μCi). Lipids are extracted, spotted on TLC glass plates (250 μm), resolved by a chloroform/methanol/water/ammonia solvent system and detected by autoradiography[2].

细胞实验

YM-201636 is dissolved in DMSO and diluted with DMEM and added to cells at a final concentration of 800 nM. Cells are treated with YM-201636 or a DMSO control for 2 h. For TER measurements cells are plated at confluency on Transwell permeable polyester filters (0.4 μM pore size) with surface area of 0.33 cm2. Media is changed ever 2-3 days and cells are grown for 7 days prior to TER measurements[4].

Cas No.

371942-69-7

分子式

C25H21N7O3

分子量

467.489

别名

YM-201636

储存和溶解度

DMSO:33 mg/mL (70.6 mM)
H2O:<1 mgml
Ethanol:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years