YM201636 is a novel PIKfyve-specific inhibitor with an IC50 of 54 nM for the net insulin response. YM201636 disrupts retroviral budding. Treatment of a Moloney leukemia virus-expressing cell line with YM201636 (800 nM) inhibits retroviral release by 80%. YM201636 (0-4 μM) significantly inhibits both basal and insulin-activated 2DG uptake in a dose-dependent manner. At concentrations as low as 160 nM, YM201636 nearly completely prevents the net insulin effect. A YM201636 concentration as high as 800 nM inhibits cell surface HA-GLUT4-eGFP accumulation by 45%. YM201636 at the concentration of 800 nM leads to a 55% inhibition of Akt-Ser473 phosphorylation and no detectable changes in total Akt. YM201636 also inhibits the insulin-dependent class IA PI 3-kinase activation at nanomolar doses. YM201636 blocks the endocytic recycling of claudin-1, providing an explanation for the intracellular accumulation. Claudin-2 is also found to constantly recycle in confluent MDCK cells and treatment with YM201636 prevents this recycling and caused accumulation of intracellular claudin-2.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 30 mg/mL|
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SF2523 is a highly selective and potent inhibitor of PI3K with IC50 values of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.
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