
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-
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).
N-[4-[1-(1,4-二氧杂螺[4.5]癸烷-8-基)-4-(8-氧杂-3-氮杂双环[3.2.1]辛烷-3-基)-1H-吡唑并[3,4-d]嘧啶-6-基]苯基]-N'-甲基脲
1144068-46-1
GSK2126458
1086062-66-9
PHA-665752
477575-56-7
TG100-115
677297-51-7