Vps34-PIK-III
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).
For research use only. We do not sell to patients.
- Purity : 99.63%
- CAS No.: 1383716-40-2
- Formula: C17H17N7
- Molecular Weight:319.36
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
-
HY-12481
SAR405Vps34 Inhibitor -
HY-12795
Vps34-IN-1Vps34 Inhibitor -
HY-12990
Spautin-1Autophagy Inhibitor -
HY-16966
SBI-0206965ULK1/AMPK Inhibitor -
HY-125169
NSC 185058ATG4B Inhibitor -
HY-114490
ULK-101ULK1 Inhibitor -
HY-101920
AutophinibVPS34 Inhibitor -
HY-100006
MRT68921NUAK1/ULK1 Inhibitor -
HY-10197
WortmanninPI3K Inhibitor -
HY-100558
Bafilomycin A1V-ATPase Inhibitor -
HY-13259
MG-132Proteasome Inhibitor -
HY-10108
LY294002PI3K Inhibitor
Publications Citing Use of MedChemExpress (MCE) Vps34-PIK-III
More- Autophagy. 2026 Jan 28:1-15. [Abstract]
- Acta Pharm Sin B. 2025 Dec 18.
- Adv Sci (Weinh). 2024 Jun;11(21):e2309315. [Abstract]
- J Transl Med. 2024 Dec 3;22(1):1095. [Abstract]
- Cell Rep. 2022 Dec 20;41(12):111868. [Abstract]
- Eur J Pharmacol. 2025 Dec 5:1008:178303. [Abstract]
- J Virol. 2024 Oct 22;98(10):e0069524. [Abstract]
- Mol Immunol. 2021 Apr:132:82-92. [Abstract]
- Front Cardiovasc Med. 2021 Sep 22:8:748156. [Abstract]
- Thorac Cancer. 2026 Mar;17(5):e70255. [Abstract]
- J Biochem. 2023 Jul 31;174(2):109-123. [Abstract]
- bioRxiv. 2025 Aug 07.
Biological Activity
Description
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) |
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. Further protocols information, click here.
-
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.
-
Cell Line:HCC cells
-
Concentration:5 µM
-
Incubation Time:24 h
-
Result:Inhibited stemness genes expression.
-
Cell Line:Huh7 and MHCC97H cells
-
Concentration:5 µM
-
Incubation Time:24 h
-
Result:Inhibited liver CSCs by activating AMPK.
In Vivo
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) Tmax (h) 0.7 Cmax (nM) 2994 AUCinf (nM•h) 2855 6725 t1/2 (h) 1.2 CL (mL/min/kg) 30 Vdss (L/kg) 1.5 F (%) 47%
Chemical Information
-
CAS No. 1383716-40-2
-
Appearance Solid
-
Molecular Weight 319.36
-
Formula C17H17N7
-
Color White to off-white
-
SMILES
NC1=NC=C(C2=CC=NC(NC3=CC=NC=C3)=N2)C(CC4CC4)=N1
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (12)
-
Journal Impact Factor
-
Most Recent
-
Autophagy
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 Oct 22;98(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 -
Solvent & Solubility
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal 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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocols
-
RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
-
Autophagy
Autophagy is a process in which eukaryotic cells use lysosomes to degrade their own cytoplasmic proteins and damaged organelles under the regulation of autophagy related gene (Atg). Microtubule-associated proteins light chain 3 (LC3) is recognized as autophagy marker, which transfers from cytoplasmic LC3 (LC3-I) to membrane type (LC3-II). LC3-II/I ratio could be detected by Western Blot and fluorescence microscopy.
-
Lysosome and acidic-vesicle live-cell staining
Lysosome and acidic-vesicle live-cell staining detects acidic intracellular compartments by using membrane-permeant acidotropic probes that accumulate in low-pH vesicles, including lysosomes, late endosomes, autolysosomes, and acidic phagosomes. LysoTracker staining is commonly used as an intensity-based readout of acidic lysosomal compartment abundance or enlargement, while acridine orange produces green fluorescence in less concentrated compartments and red fluorescence after concentration-dependent accumulation in acidic vesicular organelles. Loss or reduction of acridine-orange red signal can be used as a readout of lysosomal membrane permeabilization or reduced acidic-vesicle integrity. This protocol is designed for live cultured cells and can be adapted for fluorescence microscopy, high-content imaging, plate-reader readout, or flow cytometry when the selected literature supports the readout. Because these dyes report acidotropic accumulation rather than lysosome identity alone,
-
Liver Cancer Modeling
Liver cancer can be classified into primary liver cancer and secondary liver cancer. Secondary liver cancer is the metastatic liver cancer. Primary liver cancer includes hepatocellular carcinoma (HCC), intrahepatic cholangiocarcinoma (ICC) and fibrolamellar HCC, of which HCC is the most common form, accounting for approximately 90% of primary liver cancers[1]. HCC mouse models include chemical agent-induced models, transplanted tumor models, and genetic engineered models.
-
Macroautophagy Solutions
Macroautophagy is a conserved lysosome-dependent degradation pathway in which cytoplasmic material is sequestered into double-membrane autophagosomes and delivered to lysosomes for degradation and recycling. The pathway supports cellular homeostasis during nutrient limitation, organelle stress, protein-aggregate accumulation, infection, differentiation, and tissue remodeling by coupling cargo sequestration, autophagosome maturation, lysosomal fusion, and degradation of cargo-derived macromolecules. The core molecular sequence includes initiation by nutrient- and stress-regulated autophagy machinery, autophagosome nucleation, LC3/ATG8-family conjugation to autophagosomal membranes, cargo selection through receptors such as SQSTM1/p62, autophagosome-lysosome fusion, and lysosomal degradation. LC3 was identified as a mammalian homolog of yeast Atg8 that localizes to autophagosomal membranes after processing, and p62/SQSTM1 was shown to connect ubiquitinated cargo with autophagic degradati
Purity & Documentation
-
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)
-
Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
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.
| 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 |
Vps34-PIK-III Related Classifications
HY-12794 Related Classifications
Powered by Bioz