Art. -Nr.: HY-12795

Vps34-IN-1

17 Cited Publications

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Based on 17 publication(s) in Google Scholar

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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Reinheit: 99.79%
CAS. Nr.: 1383716-33-3
Formel: C₂₁H₂₄ClN₇O
Molecular Weight:425.91

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Vps34-IN-1 Chemical Structure

CAS. Nr.: 1383716-33-3

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Publications (17)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

Vps34

25 nM (IC₅₀)

Alle PI3K Isoform-spezifische Produkte anzeigen :

In Vitro

Vps34-IN-1 does not significantly inhibit any of the lipid kinases including class I (p110α, p110β p110γ and p110δ) and all three members of the class II PI3Ks (PI3KC2α, PI3KC2β and PI3KC2γ) enzymes^[1].
Vps34-IN-1 (0.01, 0.1, 1 μM; for 1 h) inhibits PtdIns(3)P levels at endosomes in a dose-dependent manner^[1].
Vps34-IN-1 (0.01, 0.1, 1 μM; for 1 h) induces a dose-dependent reduction in SGK3 activity that is maximally lowered by ~60% at 1 μM and ~40% at 0.1 μM. The suppression of SGK3 activity is accompanied by a commensurate decrease in T-loop and hydrophobic motif phosphorylation^[1].
Vps34-IN-1 (1, 2, 4 μM; 24 h) induces a dose-dependent inhibition of SGK3 phosphorylation^[2].

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

Western Blot Analysis^[2]

Cell Line:

MHH97H and Huh7 cells
Concentration:

1, 2, 4 μM
Incubation Time:

24 h
Result:

Induced a dose-dependent inhibition of SGK3 phosphorylation in MHH97H and Huh7 cells.
Reduced the expression of CSC-related markers CD133 and Nanog.

Chemical Information

CAS. Nr. 1383716-33-3
Appearance Solid
Molecular Weight 425.91
Formel C₂₁H₂₄ClN₇O
Color White to off-white
SMILES

CC(C)(O)CNC1=NC=C(C2=CC=NC(NC3=CC=NC(Cl)=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	1 year
	-20°C	6 months

Publications (17)

All Cell Proliferation/Viability AssayWBIFRT-PCR

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Journal Impact Factor

Autophagy

Advancing targeted protein degradation: pLIRTAC's role in glioma and CAR-T cell therapy. [Abstract]

2026 May 7:1-17. PMID: 42080372
Autophagy

Deacetylation of ATG16L1 is required for LC3-associated lysosomal microautophagy. [Abstract]

2025 Aug 28:1-15. PMID: 40851277
Nat Chem Biol

Tegavivint triggers TECR-dependent nonapoptotic cancer cell death. [Abstract]

2025 May 26. PMID: 40419770
Acta Pharm Sin B

2025 Dec 18.

Vps34-IN-1 purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2025 Dec 18.

VPS34-IN-1, VPS34-IN-2, PIK-III, and SAR405 (all 1 μM, 48 h) exhibited similar inhibition of 0.02 MOI WT SARS-CoV-2 infection in Vero E6 cells.

Vps34-IN-1 purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2025 Dec 18.

VPS34-IN-1, VPS34-IN-2, PIK-III, and SAR405 (all 1 μM, 48 h) protected cells from SARS-CoV-2-induced CPE, highlighting the critical role of VPS34 in SARS-CoV-2 infection.

Vps34-IN-1 purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2025 Dec 18.

Pharmacological profiling of VPS34 inhibitors against SARS-CoV-2 variants demonstrated that the EC50 of VPS34-IN-1 was 0.36, 0.99, 0.46, and 0.24 μM against WT, Beta, Delta, and Omicron variants, respectively.

Vps34-IN-1 purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2025 Dec 18.

Cytotoxicity assessments at 48 h in Vero E6 cells revealed that the CC50 values of VPS34-IN-1 was 11.00 μM.
J Exp Clin Cancer Res

Prolonged inhibition of class I PI3K promotes liver cancer stem cell expansion by augmenting SGK3/GSK-3β/β-catenin signalling. [Abstract]

2018 Jun 25;37(1):122. PMID: 29940988

Vps34-IN-1 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Jun 25;37(1):122. [Abstract]

Huh7 and MHCC97H cells are treated with VPS34-IN1 for 24 h, and cell lysates are subjected to western blot analysis with the indicated antibodies.
Int J Biol Sci

The SGK3/GSK3β/β-catenin signaling promotes breast cancer stemness and confers resistance to alpelisib therapy. [Abstract]

2025 Mar 19;21(6):2462-2475. PMID: 40303291
Cell Rep

HRD1 negatively regulates autolysosome formation by inhibiting liquid-liquid phase separation of SNAP29. [Abstract]

2026 Feb 24;45(2):116914. PMID: 41615796
Biochem Pharmacol

VPS34-IN1 induces apoptosis of ER + breast cancer cells via activating PERK/ATF4/CHOP pathway. [Abstract]

2023 Aug:214:115634. PMID: 37290596
Plant Cell Rep

Autophagy inducers lead to transient accumulation of autophagosomes in Arabidopsis roots. [Abstract]

2022 Feb;41(2):463-471. PMID: 34977975
PLoS Pathog

Genome-wide CRISPR/Cas9 screen identifies SLC39A9 and PIK3C3 as crucial entry factors for Ebola virus infection. [Abstract]

2024 Aug 22;20(8):e1012444. PMID: 39173055
Sports Med Health Sci

Exercise improves systemic metabolism in a monocrotaline model of pulmonary hypertension. [Abstract]

2024 Mar 8;7(1):37-47. PMID: 39649790
Thorac Cancer

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

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

2026 Jan 24.
Res Sq

A clinical drug candidate that triggers non-apoptotic cancer cell death. [Abstract]

2025 Feb 11:rs.3.rs-4138879. PMID: 39989975
bioRxiv

2024 October 31.
bioRxiv

DR5 disulfide bonding as a sensor and effector of protein folding stress. [Abstract]

2024 Mar 7:2024.03.04.583390. PMID: 38496520
Oncotarget

Simultaneous inhibition of Vps34 kinase would enhance PI3Kδ inhibitor cytotoxicity in the B-cell malignancies. [Abstract]

2016 Aug 16;7(33):53515-53525. PMID: 27447747

Vps34-IN-1 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Aug 16;7(33):53515-53525. [Abstract]

PI3KD/V-IN-01 affects autophagy HeLa cells are treated with different concentrations of PI3KD/V-IN-01, VPS34-IN-1, GDC-0941 or CAL-101 for 16 hours before they are fixed and stained for the autophagy marker LC3B.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 31 mg/mL (72.79 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

2.3479 mL

11.7396 mL

23.4791 mL

5 mM

0.4696 mL

2.3479 mL

4.6958 mL

10 mM

0.2348 mL

1.1740 mL

2.3479 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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 (5.87 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 (5.87 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 (5.87 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 (280 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]. 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]

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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3479 mL	11.7396 mL	23.4791 mL	58.6978 mL
	5 mM	0.4696 mL	2.3479 mL	4.6958 mL	11.7396 mL
	10 mM	0.2348 mL	1.1740 mL	2.3479 mL	5.8698 mL
	15 mM	0.1565 mL	0.7826 mL	1.5653 mL	3.9132 mL
	20 mM	0.1174 mL	0.5870 mL	1.1740 mL	2.9349 mL
	25 mM	0.0939 mL	0.4696 mL	0.9392 mL	2.3479 mL
	30 mM	0.0783 mL	0.3913 mL	0.7826 mL	1.9566 mL
	40 mM	0.0587 mL	0.2935 mL	0.5870 mL	1.4674 mL
	50 mM	0.0470 mL	0.2348 mL	0.4696 mL	1.1740 mL
	60 mM	0.0391 mL	0.1957 mL	0.3913 mL	0.9783 mL

Keywords

Vps34-IN-1

17 Cited Publications

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Vps34-IN-1

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Publications Citing Use of MedChemExpress (MCE) Vps34-IN-1

Alle PI3K Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (17)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Vps34-IN-1 Related Classifications

HY-12795 Related Classifications