YM201636 potently inhibits mammalian PIKfyve with an IC50 of 33 nM but not yeast orthologue Fab1 with an IC50 of >5 ¦ÌM, exhibiting around 100-fold selectivity for PtdIns3P p110¦Á with an IC50 of 3 ¦ÌM. YM201636 (0.8 ¦ÌM) significantly decreases the production of PtdIns(3,5)P2 by 80% in serum-starved NIH3T3 cells followed by serum stimulation with no effect on serum-stimulated protein kinase B (PKB) Ser 473 phosphorylation. YM-201636 reversibly impairs endosomal trafficking in NIH3T3 cells by blocking PIKfyve and PtdIns(3,5)P2 production, mimicking the effect produced by depleting PIKfyve with siRNA. YM-201636 (0.8 ¦ÌM) also significantly reduces retroviruses budding from cells by 80%, apparently through interfering with the endosomal sorting complex required for transport (ESCRT) machinery.

June 21, 2017

prudect name : YM201636 potently inhibits mammalian PIKfyve with an IC50 of 33 nM but not yeast orthologue Fab1 with an IC50 of >5 ¦ÌM, exhibiting around 100-fold selectivity for PtdIns3P p110¦Á with an IC50 of 3 ¦ÌM. YM201636 (0.8 ¦ÌM) significantly decreases the production of PtdIns(3,5)P2 by 80% in serum-starved NIH3T3 cells followed by serum stimulation with no effect on serum-stimulated protein kinase B (PKB) Ser 473 phosphorylation. YM-201636 reversibly impairs endosomal trafficking in NIH3T3 cells by blocking PIKfyve and PtdIns(3,5)P2 production, mimicking the effect produced by depleting PIKfyve with siRNA. YM-201636 (0.8 ¦ÌM) also significantly reduces retroviruses budding from cells by 80%, apparently through interfering with the endosomal sorting complex required for transport (ESCRT) machinery.
YM 201636

Synonyms: CAS NO: 371942-69-7Molecular Formula: C₂₅H₂₁N₇O₃Molecular Weight: 467.48Purity: 98% minSolubility: In DMSOStorage: -20°C

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