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Administration of VPS34-IN1 to cells induces a rapid dose-dependent dispersal of a specific PtdIns(3)P-binding probe from endosome membranes, within 1min, without affecting the ability of class I PI3K to regulate Akt. It can also induce a rapid ~50-60% loss of SGK3 phosphorylation within 1min. VPS34-IN1 has no inhibition to the SGK2 isoform that does not possess a PtdIns(3)P-binding PX domain.
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Source | Biochem J (2014). Figure 3. VPS34-IN1 |
| Method | Immunofluorescence and time-lapse microscopy | |
| Cell Lines | U2OS cell line | |
| Concentrations | 1.0 μM | |
| Incubation Time | 1 h | |
| Results | Treatment with Vps34-IN1 for 1 h induced a marked dose-dependent suppression of endosomal localization of GFP–2×FYVEHrs with ~80% loss observed at 1.0 μM and ~50% loss at 0.1 μM |
| Molecular Weight | 425.91 |
| Formula | C21H24ClN7O |
| CAS Number | 1383716-33-3 |
| Solubility (25°C) | 65 mg/mL in DMSO |
| 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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