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.
|Source||Biochem J (2014). Figure 3. VPS34-IN1|
|Method||Immunofluorescence and time-lapse microscopy|
|Cell Lines||U2OS cell line|
|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|
|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||85 mg/mL in DMSO|
Cinderella finds her shoe: the first Vps34 inhibitor uncovers a new PI3K-AGC protein kinase connection.
Bilanges B, et al. Biochem J. 2014 Dec 1;464(2):e7-10. PMID: 25395352.
Characterization of VPS34-IN1, a selective inhibitor of Vps34, reveals that the phosphatidylinositol 3-phosphate-binding SGK3 protein kinase is a downstream target of class III phosphoinositide 3-kinase.
Bago R, et al. Biochem J. 2014 Nov 1;463(3):413-27. PMID: 25177796.
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