371942-69-7

YM201636

371942-69-7

编号ABP000099 化学名称YM201636 英文名称 YM201636 分子式C25H21N7O3 分子量467.4793 纯度 >99%

化学名称 : YM201636

CAS : 371942-69-7

英文名称: YM201636

英文同义词: 6-Amino-N-[3-[4-(4-morpholinyl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]phenyl]-3-pyridinecarboxamide

溶解度:DMSO

储存条件:-20C 2 years

生物活性

A cell-permeable pyridofuropyrimidine compound that selectively inhibits mammalian type III PtdInsP kinase (IC50 = 33 nM and >5 µM using murine PIKfyve and yeast Fab1, respectively), while exhibiting much reduced activity against p110α (IC50 = 3.3 µM) and little activity against type IIγ PtdInsP kinase even at concentrations as high as 10 µM. Shown to block serum-induced PtdIns(3,5)P2 production in NIH3T3 cells (80% inhibition at 800 nM) and disrupt cellular endosomal transport in a reversible manner.

参考文献

Ikonomov, O.C., Sbrissa, D., Shisheva, A.. YM201636, an inhibitor of retroviral budding and PIKfyve-catalyzed PtdIns(3,5)P2 synthesis, halts glucose entry by insulin in adipocytes. Biochem Biophys Res Commun 382 566-570 (2009).

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 Rep 9(2) 164-170 (2008).

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