Art. -Nr.: HY-12794

Vps34-PIK-III

12 Cited Publications

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Based on 12 publication(s) in Google Scholar

Vps34-PIK-III is an orally active and selective VPS34 inhibitor (IC₅₀=18 nM). Vps34-PIK-III effectively inhibits autophagy and can be used as a molecular tool. vps34-PIK-III is also a PI3K inhibitor that inhibits the expression of genes in liver cancer stem cells (CSCs).

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Reinheit: 99.63%
CAS. Nr.: 1383716-40-2
Formel: C₁₇H₁₇N₇
Molecular Weight:319.36

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Vps34-PIK-III Chemical Structure

CAS. Nr.: 1383716-40-2

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (12)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[2]

Vps34

18 nM (IC₅₀)

PI(3)Kδ

1.2 μM (IC₅₀)

PI(3)Kγ

3.04 μM (IC₅₀)

PI(3)Kα

3.96 μM (IC₅₀)

Alle PI3K Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
U2OS	IC₅₀	12 nM Compound: PIK-III	Inhibition of VPS34 in human U2OS cells incubated for 2 hrs by GFP-FYVE reporter gene assay Inhibition of VPS34 in human U2OS cells incubated for 2 hrs by GFP-FYVE reporter gene assay	[PMID: 26819669]

In Vitro

Vps34-PIK-III (1, 5, 10 μM; 24 h) inhibits autophagy and LC3 lipidation in DLD1 cells^[1].
Vps34-PIK-III (1, 5, 10 μM; 24 h) leads to an increase in the lipidated and nonlipidated forms of LC3 in DLD1 cells^[1].
Vps34-PIK-III (5 μM; 24 h) significantly decreases the expression of stemness genes in HCC cells^[2].
Vps34-PIK-III (5 μM; 24 h) suppresses liver CSCs via AMPK activation in Huh7 and MHCC97H cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

DLD1 cells
Concentration:

1, 5, 10 µM
Incubation Time:

24 h
Result:

Prevented the degradation of autophagy substrates p62, NCOA4, NBR1, NDP52, and FTH1.

RT-PCR^[1]

Cell Line:

HCC cells
Concentration:

5 µM
Incubation Time:

24 h
Result:

Inhibited stemness genes expression.

Western Blot Analysis^[1]

Cell Line:

Huh7 and MHCC97H cells
Concentration:

5 µM
Incubation Time:

24 h
Result:

Inhibited liver CSCs by activating AMPK.

In Vivo

Vps34-PIK-III (10 mg/kg; p.o.; single) rapidly absorbed and shows moderate mean systemic clearance (30 mL/min/kg, approximately 33% of hepatic blood flow), with good oral bioavailability (F% = 47)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

C57BL/6 mice^[1].
Dosage:

10 mg/kg; 2 mg/kg
Administration:

Oral administration; intravenous injection; single
Result:

1.19 Pharmacokinetic Parameters of Vps34-PIK-III in C57BL/6 mice^[1].

IV (2 mg/kg) PO (10 mg/kg)

T_max (h) 0.7

C_max (nM) 2994

AUC_inf (nM•h) 2855 6725

t_1/2 (h) 1.2

CL (mL/min/kg) 30

Vdss (L/kg) 1.5

F (%) 47%

Chemical Information

CAS. Nr. 1383716-40-2
Appearance Solid
Molecular Weight 319.36
Formel C₁₇H₁₇N₇
Color White to off-white
SMILES

NC1=NC=C(C2=CC=NC(NC3=CC=NC=C3)=N2)C(CC4CC4)=N1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (12)

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Journal Impact Factor

Acta Pharm Sin B

2025 Dec 18.
Autophagy

Deubiquitinase USP15 restricts LC3-dependent targeting of Mycobacterium tuberculosis. [Abstract]

2026 Jan 28:1-15. PMID: 41606832
Adv Sci (Weinh)

Dual Activity of Type III PI3K Kinase Vps34 is Critical for NK Cell Development and Senescence. [Abstract]

2024 Jun;11(21):e2309315. PMID: 38544346
J Transl Med

Doxorubicin synergizes bortezomib-induced multiple myeloma cell death by inhibiting aggresome formation and augmenting endoplasmic reticulum/Golgi stress and apoptosis. [Abstract]

2024 Dec 3;22(1):1095. PMID: 39623468
Cell Rep

The Golgi-resident protein ACBD3 concentrates STING at ER-Golgi contact sites to drive export from the ER. [Abstract]

2022 Dec 20;41(12):111868. PMID: 36543137
Eur J Pharmacol

Doxorubicin-mediated retardation of aggresome formation enhances Carfilzomib-induced cell death synergistically by augmenting ER stress and proapoptotic signaling. [Abstract]

2025 Dec 5:1008:178303. PMID: 41183585
J Virol

The class III phosphatidylinositol 3-kinase VPS34 supports EV71 replication by promoting viral replication organelle formation. [Abstract]

2024 Sep 10:e0069524. PMID: 39254312
Mol Immunol

Eva1a inhibits NLRP3 activation to reduce liver ischemia-reperfusion injury via inducing autophagy in kupffer cells. [Abstract]

2021 Apr:132:82-92. PMID: 33556710
Front Cardiovasc Med

Samm50 Promotes Hypertrophy by Regulating Pink1-Dependent Mitophagy Signaling in Neonatal Cardiomyocytes. [Abstract]

2021 Sep 22:8:748156. PMID: 34631840
Thorac Cancer

Effects of Autophagy Inhibition by SAR405, a Selective VPS34 Inhibitor, on Pleural Mesothelioma Cells. [Abstract]

2026 Mar;17(5):e70255. PMID: 41771171
J Biochem

A lipid scramblase TMEM41B is involved in the processing and transport of GPI-anchored proteins. [Abstract]

2023 Jul 31;174(2):109-123. PMID: 37279648
bioRxiv

2025 Aug 07.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 31 mg/mL (97.07 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.1313 mL

15.6563 mL

31.3126 mL

5 mM

0.6263 mL

3.1313 mL

6.2625 mL

10 mM

0.3131 mL

1.5656 mL

3.1313 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (7.83 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (7.83 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (7.83 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Honda A, et al. Potent, Selective, and Orally Bioavailable Inhibitors of VPS34 Provide Chemical Tools to Modulate Autophagy in Vivo. ACS Med Chem Lett. 2015 Nov 13;7(1):72-6. [Content Brief]

[2]. Liu F, et al. PIK3C3 regulates the expansion of liver CSCs and PIK3C3 inhibition counteracts liver cancer stem cell activity induced by PI3K inhibitor. Cell Death Dis. 2020 Jun 8;11(6):427. [Content Brief]

[3]. Dowdle WE, et al. Selective VPS34 inhibitor blocks autophagy and uncovers a role for NCOA4 in ferritin degradation and iron homeostasis in vivo. Nat Cell Biol. 2014 Nov;16(11):1069-79. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.1313 mL	15.6563 mL	31.3126 mL	78.2816 mL
	5 mM	0.6263 mL	3.1313 mL	6.2625 mL	15.6563 mL
	10 mM	0.3131 mL	1.5656 mL	3.1313 mL	7.8282 mL
	15 mM	0.2088 mL	1.0438 mL	2.0875 mL	5.2188 mL
	20 mM	0.1566 mL	0.7828 mL	1.5656 mL	3.9141 mL
	25 mM	0.1253 mL	0.6263 mL	1.2525 mL	3.1313 mL
	30 mM	0.1044 mL	0.5219 mL	1.0438 mL	2.6094 mL
	40 mM	0.0783 mL	0.3914 mL	0.7828 mL	1.9570 mL
	50 mM	0.0626 mL	0.3131 mL	0.6263 mL	1.5656 mL
	60 mM	0.0522 mL	0.2609 mL	0.5219 mL	1.3047 mL
	80 mM	0.0391 mL	0.1957 mL	0.3914 mL	0.9785 mL

Keywords

Vps34-PIK-III

12 Cited Publications

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	IV (2 mg/kg)	PO (10 mg/kg)
T_max (h)		0.7
C_max (nM)		2994
AUC_inf (nM•h)	2855	6725
t_1/2 (h)	1.2
CL (mL/min/kg)	30
Vdss (L/kg)	1.5
F (%)		47%

Vps34-PIK-III

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Glucose Metabolism Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Cell Death Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Vps34-PIK-III

Alle PI3K Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (12)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Vps34-PIK-III Related Classifications

HY-12794 Related Classifications