Home PI3K/Akt/mTOR PI3K inhibitor VPS34 inhibitor 1 (Compound 19) For research use only.

VPS34 inhibitor 1 (Compound 19)

Synonyms: PIK-III analogue

VPS34 inhibitor 1 (Compound 19, PIK-III analogue) is a potent and selective inhibitor of VPS34 with an IC50 of 15 nM.

VPS34 inhibitor 1 (Compound 19) Chemical Structure

VPS34 inhibitor 1 (Compound 19) Chemical Structure

CAS No. 1383716-46-8

Purity & Quality Control

VPS34 inhibitor 1 (Compound 19) Related Products

Signaling Pathway

PI3K Signaling Pathways

PI3K Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
U2OS Function assay 2 hrs Inhibition of VPS34 in human U2OS cells incubated for 2 hrs by GFP-FYVE reporter gene assay, IC50=0.025μM 26819669
DLD1 Function assay 1 to 10 uM 24 hrs Inhibition of VPS34 in human DLD1 cells assessed as prevention of NCOA4 protein degradation at 1 to 10 uM incubated for 24 hrs by Western blot analysis 26819669
DLD1 Function assay 1 to 10 uM 24 hrs Inhibition of VPS34 in human DLD1 cells assessed as prevention of p62 degradation at 1 to 10 uM incubated for 24 hrs by Western blot analysis 26819669
DLD1 Function assay 1 to 10 uM 24 hrs Inhibition of VPS34 in human DLD1 cells assessed as prevention of NBR1 protein degradation at 1 to 10 uM incubated for 24 hrs by Western blot analysis 26819669
DLD1 Function assay 1 to 10 uM 24 hrs Inhibition of VPS34 in human DLD1 cells assessed as prevention of NDP52 protein degradation at 1 to 10 uM incubated for 24 hrs by Western blot analysis 26819669
DLD1 Function assay 1 to 10 uM 24 hrs Inhibition of VPS34 in human DLD1 cells assessed as prevention of FTH1 protein degradation at 1 to 10 uM incubated for 24 hrs by Western blot analysis 26819669
DLD1 Function assay 1 to 10 uM 24 hrs Inhibition of VPS34 in human DLD1 cells assessed as increase in LC3-1 protein expression at 1 to 10 uM incubated for 24 hrs by Western blot analysis 26819669
DLD1 Function assay 1 to 10 uM 24 hrs Inhibition of VPS34 in human DLD1 cells assessed as increase in LC3-2 protein expression at 1 to 10 uM incubated for 24 hrs by Western blot analysis 26819669
Click to View More Cell Line Experimental Data

Biological Activity

Description VPS34 inhibitor 1 (Compound 19, PIK-III analogue) is a potent and selective inhibitor of VPS34 with an IC50 of 15 nM.
Targets
VPS34 [1]
(Cell-free assay)
15 nM
In vitro
In vitro Compound 19 is extraordinarily selective over other lipid and protein kinases. The ability of compound 19 to prevent the degradation of autophagy substrates p62, NCOA4, NBR1, NDP52, and FTH1 is similar to PIK-III. In addition, treatment of cells with compound 19 leads to an increase in the lipidated and nonlipidated forms of LC3 similar to previous reports using PIK-III[1].
Cell Research Cell lines U2OS cells
Concentrations 0, 1, 5, 10 μM
Incubation Time 24 h
Method For inhibitor assay, cells are plated and the following day when cells had reached 90%, are treated with dimethyl sulfoxide (DMSO, vehicle) or the indicated concentration of PIK-III or Compound 19, both dissolved in DMSO. 24 hours later, cells are lysed in RIPA supplemented with 1% SDS and mini-EDTA protease inhibitors, homogenized by passage through a Qiashredder column and the protein is quantified by DC Lowry protein assay.
In Vivo
In vivo The pharmacokinetic profile of analogue 19 is determined in C57BL/6 mice. After oral administration at 10 mg/kg, the compound is rapidly absorbed and showed moderate mean systemic clearance (30 mL/min/kg, approximately 33% of hepatic blood flow), with good oral bioavailability (F% = 47). Based on these PK parameters and the cellular activity, compound 19 constitutes a suitable candidate for in vivo studies. Upon oral administration of compound 19 at 50 mg/kg twice a day (BID) for 7 days, LC3-II accumulates consistent with reduced autophagic capacity in time-dependent manner. It inhibits autophagy in vivo[1].
Animal Research Animal Models C57BL/6 Mice
Dosages 10 mg/kg(p.o.) or 2 mg/kg(I.V.)
Administration oral administration or I.V.

Chemical Information & Solubility

Molecular Weight 391.47 Formula

C21H25N7O
CAS No. 1383716-46-8 SDF Download VPS34 inhibitor 1 (Compound 19) SDF
Smiles CC(C)(CNC1=NC=C(C(=N1)CC2CC2)C3=NC(=NC=C3)NC4=CC=NC=C4)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 78 mg/mL ( (199.24 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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