Vps34-IN-1

Vps34-IN-1 is a potent and selective inhibitor of class III Vps34 PI3K. Vps34-IN-1 inhibits phosphorylation of PtdIns by recombinant insect cell expressed Vps34-Vps15 complex with an IC50 of ~25 nM. Vps34-IN-1 can suppress SGK3 activation by reducing PtdIns (3) P levels via lowering phosphorylation of T-loop and hydrophobic motifs. Vps34-IN-1 modulates autophagy[1][2][3].

Product Specifications

CAS Number

[1383716-33-3]

UNSPSC

12352005

Hazard Statement

H302

Target

Autophagy; PI3K

Type

Reference compound

Related Pathways

Autophagy; PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Vps34-IN-1.html

Purity

99.79

Solubility

DMSO : ≥ 31 mg/mL

Smiles

CC(C)(O)CNC1=NC=C(C2=CC=NC(NC3=CC=NC(Cl)=C3)=N2)C(CC4CC4)=N1

Molecular Formula

C21H24ClN7O

Molecular Weight

425.91

Precautions

H302

References & Citations

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