1383716-33-3
Chemical Structure
Vps34-IN-1
- CAS No.: 1383716-33-3
- Formula:C21H24ClN7O
- Molecular Weight:425.91
IUPAC Name: 1-((2-((2-chloropyridin-4-yl)amino)-4'-(cyclopropylmethyl)-[4,5'-bipyrimidin]-2'-yl)amino)-2-methylpropan-2-ol
InChIKey: AWNXKZVIZARMME-UHFFFAOYSA-N
SMILES: CC(C)(O)CNC1=NC=C(C2=CC=NC(NC3=CC=NC(Cl)=C3)=N2)C(CC4CC4)=N1
Biological Activity: 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].
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Vps34-IN-1 | 99.79% | 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. | ||||||||||||||||||||
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- [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. [Content Brief]
- [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. [Content Brief]
- [3]. Limpert AS, et al. Autophagy in Cancer: Regulation by Small Molecules. Trends Pharmacol Sci. 2018 Dec;39(12):1021-1032 [Content Brief]
Keywords
