Home PI3K/Akt/mTOR PI3K inhibitor VPS34 inhibitor 1 (Compound 19)

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VPS34 inhibitor 1 (Compound 19) PI3K inhibitor

Cat.No.S8456

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) PI3K inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 391.47

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Quality Control

Batch: Purity: 99.27%
99.27

Cell Culture, Treatment & Working Concentration

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
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Solubility

In vitro
Batch:

DMSO : 78 mg/mL (199.24 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 391.47 Formula

C21H25N7O

 Storage (From the date of receipt)
CAS No. 1383716-46-8 Download SDF Storage of Stock Solutions

Synonyms PIK-III analogue Smiles CC(C)(CNC1=NC=C(C(=N1)CC2CC2)C3=NC(=NC=C3)NC4=CC=NC=C4)O

Mechanism of Action

Targets/IC50/Ki
VPS34
(Cell-free assay)
15 nM
In vitro
VPS34 inhibitor 1 (Compound 19) is extraordinarily selective over other lipid and protein kinases, and its ability to prevent the degradation of autophagy substrates p62, NCOA4, NBR1, NDP52, and FTH1 is similar to PIK-III. In addition, treatment of cells with this compound leads to an increase in the lipidated and nonlipidated forms of LC3 similar to previous reports using PIK-III.
In vivo
The pharmacokinetic profile of VPS34 inhibitor 1 (Compound 19) is determined in C57BL/6 mice. After oral administration at 10 mg/kg, it 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, this compound constitutes a suitable candidate for in vivo studies. Upon oral administration 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.
References

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