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CAS No.: 371942-69-7

YM-201636 Catalog No. CSN15968

Synonyms: YM-201636

YM-201636 is a selective PIKfyve inhibitor with IC50 of 33 nM.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 PIKfyve

IC50:33nM
描述PIKfyve is the mammalian type III PtdInsP kinase that acts on PtdIns3P (phosphatidylinositol 3-phosphate) to generate PtdIns(3,5)P₂. PtdIns(3,5)P₂ has been shown to have a role in the retrieval of cargoes to the trans-Golgi network (TGN), and has been implicated in insulin-regulated IRAP/GLUT4 vesicle transport. YM201636 is a novel, potent and selective inhibitor of PIKfyve, with a half-maximal inhibitory concentration (IC₅₀) of 33 nM. An IC₅₀ for PtdIns3P p110α was determined to be 3 μM, almost 100-fold higher than for PIKfyve. In serum-starved NIH3T3 cells, YM201636 at 800 nM decreased PtdIns(3,5)P₂ production by 80%. Acute treatment with YM201636 of various cell types, including mouse embryonic fibroblasts (MEFs), Madin–Darby canine kidney (MDCK), MCF10A, COS7 and NIH3T3 cells, caused the formation of large vesicular structures. The size and rate of formation are time- and concentration-dependent, with an A₅₀ of around 400 nM. In NIH3T3 cells treated with 800 nM YM201636 for 2 h, YM201636 became concentrated on the surface of a subset of enlarged vesicular structures and on some lumenal vesicles. When NIH3T3 cells were treated with YM201636, it was apparent that most of LC3 (the GFP(green fluorescent protein)-tagged autophagosome marker) accumulated inside the enlarged vesicles^[2]. YM201636 almost completely inhibited basal and insulin-activated 2-deoxyglucose uptake at doses as low as 160 nM, with an IC_{50_{of 54 nM for the net insulin response. In addition to PIKfyve, YM201636 also completely inhibited insulin-dependent activation of class IA PI 3-kinase^[3].}}
参考文献

[1] Sbrissa D, Ikonomov OC, et al. Functional dissociation between PIKfyve-synthesized PtdIns5P and PtdIns(3,5)P2 by means of the PIKfyve inhibitor YM201636. Am J Physiol Cell Physiol. 2012 Aug 15;303(4):C436-46.
[2] A selective PIKfyve inhibitor blocks PtdIns(3,5)P(2) production and disrupts endomembrane transport and retroviral budding
[3] YM201636, an inhibitor of retroviral budding and PIKfyve-catalyzed PtdIns(3,5)P2 synthesis, halts glucose entry by insulin in adipocytes

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1391 mL
- 10.6957 mL
- 21.3913 mL
- 5 mM
- 0.4278 mL
- 2.1391 mL
- 4.2783 mL
- 10 mM
- 0.2139 mL
- 1.0696 mL
- 2.1391 mL

技术信息

CAS号

371942-69-7

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H21N7O3

运输

蓝冰

分子量

467.48

别名

YM-201636

溶解度

DMSO	35.0 mg/mL (74.9 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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