Vps34-IN-1

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Chemical Structure| 1383716-33-3 同义名 : Vacuolar Protein Sorting 34 Inhibitor 1; Vps34 Inhibitor 1; VPS34IN1, VPS34 IN1, VPS34-IN1
CAS号 : 1383716-33-3
货号 : A194997
分子式 : C21H24ClN7O
纯度 : 98%
分子量 : 425.91
MDL号 : MFCD28963905
存储条件：

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(70.44 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • Vps34

    Vps34, IC50:25 nM
描述 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 [1][2][3].
作用机制 Vps34-IN-1inhibits Vps34 signaling pathway via rapid perturbation of PtdIns(3)P synthesis at endosomal membrane.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.35mL

0.47mL

0.23mL

11.74mL

2.35mL

1.17mL

23.48mL

4.70mL

2.35mL
参考文献

[1]Ruzica Bago, et al. 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. Biochem J. 2014 Nov 1;463(3):413-27.

[2]Fengchao Liu, et al. Prolonged inhibition of class I PI3K promotes liver cancer stem cell expansion by augmenting SGK3/GSK-3β/β-catenin signaling. J Exp Clin Cancer Res. 2018 Jun 25;37(1):122.

[3]Limpert AS, et al. Autophagy in Cancer: Regulation by Small Molecules. Trends Pharmacol Sci. 2018 Dec;39(12):1021-1032