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YM201636

现货
Catalog No.
B2189
PIKfyve抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,000.00
现货
5mg
¥ 960.00
现货
10mg
¥ 1,700.00
现货
50mg
¥ 6,450.00
现货
100mg
¥ 11,000.00
现货

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Background

YM201636 is a potent, selective and cell-permeable inhibitor of mammalian class III phosphatidylinositol phosphate kinase PIKfyve with IC50 value of 33nM [1].

The pyridofuropyrimidine compound, YM201636, is a small-molecule inhibitor of PIKfyve. In the in vitro assay, it inhibits PIKfyve with IC50 value of 33nM and shows no inhibition of yeast orthologue of PIKfyve. It inhibits PtdIns3P p110α and type Iα PtdInsP kinase with IC50 values of 3μM and > 2μM, respectively. The type IIγ PtdInsP kinase is found to be insensitive to YM201636. In serum-starved NIH3T3 cells, YM201636 inhibits PtdIns (3, 5) P2 production by 80% at concentration of 800nM. Acute treatment of YM201636 to MEFs, MDCK, MCF10A, COS7 and NIH3T3 cells causes the formation of large vesicular structures. Besides that, YM201636 is also found to reduce the Akt phosphorylation and GLUT4 cell surface translocation through inhibiting the insulin-dependent class I PI 3k activation [1, 2].

References:
[1] Jefferies H B J, Cooke F T, Jat P, et al. A selective PIKfyve inhibitor blocks PtdIns (3, 5) P2 production and disrupts endomembrane transport and retroviral budding. EMBO reports, 2008, 9(2): 164-170.
[2] Ikonomov O C, Sbrissa D, Shisheva A. YM201636, an inhibitor of retroviral budding and PIKfyve-catalyzed PtdIns (3, 5) P2synthesis, halts glucose entry by insulin in adipocytes. Biochemical and biophysical research communications, 2009, 382(3): 566-570.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt467.48
Cas No.371942-69-7
FormulaC25H21N7O3
Solubility≥11.68mg/mL in DMSO
Chemical Name6-amino-N-[3-(4-morpholin-4-ylpyrido[2,3]furo[2,4-b]pyrimidin-2-yl)phenyl]pyridine-3-carboxamide
SDFDownload SDF
Canonical SMILESC1COCCN1C2=NC(=NC3=C2OC4=C3C=CC=N4)C5=CC(=CC=C5)NC(=O)C6=CN=C(C=C6)N
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1, 2]:

细胞系

小鼠3T3L1脂肪细胞,NIH3T3细胞

溶解方法

该化合物在DMSO中的溶解度>11.7mg/mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

0-4 μM给药30分钟或800 nM给药2h

应用

在小鼠3T3L1脂肪细胞中,YM201636以剂量依赖性方式显著抑制基础和胰岛素激活的2DG摄取。 YM201636(160nM)几乎完全抑制了胰岛素效应,在54±4nM下具有50%的抑制作用。 800nM的YM201636产生细胞表面HA-GLUT4-eGFP积累的45%抑制和Akt-Ser473磷酸化的55%抑制。在NIH3T3细胞中,800nM的YM201636将PtdIns(3,5)P2产量降低80%。YM201636通过影响PIKfyve和PtdIns(3,5)P2生产诱导囊泡表型。

References:

[1] Jefferies H B J, Cooke F T, Jat P, et al. A selective PIKfyve inhibitor blocks PtdIns (3, 5) P2 production and disrupts endomembrane transport and retroviral budding. EMBO reports, 2008, 9(2): 164-170.

[2]. Ikonomov O C, Sbrissa D, Shisheva A. YM201636, an inhibitor of retroviral budding and PIKfyve-catalyzed PtdIns (3, 5) P2synthesis, halts glucose entry by insulin in adipocytes. Biochemical and biophysical research communications, 2009, 382(3): 566-570.

生物活性

Description YM201636是一种PIKfyve的选择性抑制剂,IC50值为33 nM.
靶点 PIKfyve p110α        
IC50 33 nM 3.3 μM        

质量控制