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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 |
|---|
| AS605240
AS-605240 is a potent and selective inhibitor of PI 3-kinase γ (PI3Kγ) with an IC50 of 8 nM. |
| BEZ235
BEZ235 (NVP-BEZ235) is a potent dual PI3K and mTOR inhibitor of p110α, p110γ, p110δ and p110β with IC50 of 4 nM, 5 nM, 7 nM and 75 nM, respectively. |
| BKM120 (Buparlisib)
BKM120 (NVP-BKM120) is a potent and highly specific oral pan-class I PI3K inhibitor. |
| GDC-0941 (Pictilisib)
GDC-0941 is a selective and potent inhibitor of Class I PI3K, p110a IC50=0.003uM, U87MG IC50=0.95μM. |
| AS-252424
AS-252424 is a furan-2-ylmethylene thiazolidinedione as a selective ATP-competitive PI3Kγ inhibitor with IC50 with 33 nM. |
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