Vps34-IN-1

Vps34-IN-1 is a powerful and specific inhibitor targeting class III Vps34 PI3K. It impedes the phosphorylation of PtdIns by the recombinant insect cell-expressed Vps34-Vps15 complex, with an IC50 of approximately 25 nM. Additionally, Vps34-IN-1 can hinder SGK3 activation by decreasing PtdIns(3)P levels, thereby reducing phosphorylation of T-loop and hydrophobic motifs. Furthermore, Vps34-IN-1 regulates autophagy ¹²³.

Vps34-IN-1 exhibits no substantial inhibition of lipid kinases, including class I (p110α, p110β, p110γ, and p110δ) and all three members of class II PI3Ks (PI3KC2α, PI3KC2β, and PI3KC2γ) enzymes ¹.

Vps34-IN-1 (0.01, 0.1, 1 μM; for 1 h) suppresses PtdIns(3)P levels at endosomes in a dose-dependent fashion ¹.

Vps34-IN-1 (0.01, 0.1, 1 μM; for 1 h) elicits a dose-dependent decline in SGK3 activity, reaching a maximum reduction of approximately 60% at 1 μM and approximately 40% at 0.1 μM. This decrease in SGK3 activity correlates with a proportional decrease in phosphorylation of both the T-loop and hydrophobic motif ¹.

Vps34-IN-1 (1, 2, 4 μM; 24 h) triggers a dose-dependent suppression of SGK3 phosphorylation ².

溶解方案(细胞实验)

DMSO 中的溶解度 : ≥ 31 mg/mL (72.79 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)|* "≥" means soluble, but saturation unknown.

溶解方案(动物实验)

"方案 一": "请依序添加每种溶剂：10% DMSO 40% PEG300 5% Tween-80 45% SalineSolubility: ≥ 2.5 mg/mL (5.87 mM); 澄清溶液 此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。"

"方案 二": "请依序添加每种溶剂：10% DMSO 90% (20% SBE-β-CD in Saline)Solubility: ≥ 2.5 mg/mL (5.87 mM); 澄清溶液 此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。"

"方案 三": "请依序添加每种溶剂：10% DMSO 90% Corn OilSolubility: ≥ 2.5 mg/mL (5.87 mM); 澄清溶液 此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。"