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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 |
| Related PI3K Products |
|---|
| PI3Kγ inhibitor AZ2
PI3Kγ inhibitor AZ2 is a highly selective PI3Kγ inhibitor (The pIC50 value for PI3Kγ is 9.3). |
| NIBR-17
NIBR-17 is a pan-class I PI3K inhibitor with suitable pharmacokinetic properties and inhibits tumor growth. |
| RV-1729
RV-1729 is an inhibitor of the phosphatidylinositol 3-kinase-δ (PI3Kδ). |
| Vulolisib
Vulolisib is a potent and orally active phosphatidylinositol 3-kinase (PI3K) inhibitor, with IC50 values of 0.2 nM, 168 nM, 90 nM and 49 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. |
| Vps34-IN-4
Vps34-IN-4 is a potent, selective, and orally active inhibitor of VPS34. |
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