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YM-201636

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Chemical Structure| 371942-69-7 同义名 : -
CAS号 : 371942-69-7
货号 : A213349
分子式 : C25H21N7O3
纯度 : 98%
分子量 : 467.479
MDL号 : MFCD16038303
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 45 mg/mL(96.26 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • p110α

    p110α, IC50:3.3 μM
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 IC50 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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.14mL

0.43mL

0.21mL

10.70mL

2.14mL

1.07mL

21.39mL

4.28mL

2.14mL
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