371942-69-7
371942-69-7
Chemical Name : YM201636
CAS : 371942-69-7
Synonyms: 6-Amino-N-[3-[4-(4-morpholinyl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]phenyl]-3-pyridinecarboxamide
Solubility:DMSO
Storage:-20C 2 years
Biologieal
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.
Reference
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).
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