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.
| Molecular Weight | 467.48 |
| Formula | C25H21N7O3 |
| CAS Number | 371942-69-7 |
| Solubility (25°C) | DMSO 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
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