Vps34-IN-4
Based on 1 Customer Validation
Vps34-IN-4 is an orally active and selective VPS34 inhibitor with an IC50 of 15 nM against human VPS34. Vps34-IN-4 binds to the ATP-binding pocket of VPS34. Vps34-IN-4 inhibits autophagy (autophagy) by blocking the degradation of autophagic substrates and increasing both lipidated and non-lipidated forms of LC3. Vps34-IN-4 induces time-dependent LC3-II accumulation in tumor tissues of tumor-bearing mice. Vps34-IN-4 can be used for research on cancers such as colon cancer.
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- Purity : 98.79%
- CAS No.: 1383716-46-8
- 화학식: C21H25N7O
- 분자량:391.47
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
제품 설명
IC50 & Target
[1]|
hVps34 15 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| U2OS | IC50 |
25 nM
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Inhibition of VPS34-dependent phosphatidylinositol-3-phosphate production in cells measured via GFP-FYVE reporter cellular assay.
Inhibition of VPS34-dependent phosphatidylinositol-3-phosphate production in cells measured via GFP-FYVE reporter cellular assay.
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26819669 |
In Vitro
Vps34-IN-4 (Compound 19) (1-10 μM; 24 h) potently inhibits autophagy in DLD1 cells and induces concentration-dependent accumulation of autophagic substrates and LC3[1].
Vps34-IN-4 potently inhibits VPS34 activity in U2OS cells with an IC50 of 25 nM in the GFP-FYVE reporter assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:DLD1 human colon cancer cells
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Concentration:1, 5, 10 μM
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Incubation Time:24 h
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Result:Caused a concentration-dependent increase in the protein levels of autophagy cargo receptors NBR1, NCOA4, SQSTM1/p62, NDP52, and ferritin heavy chain (FTH1).
Caused a concentration-dependent increase in both the lipidated (LC3-II) and nonlipidated (LC3-I) forms of LC3.
Showed no change in GAPDH levels across conditions, serving as a loading control.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice (tumor-bearing; C57BL/6 mice used for PK only)[1]
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Dosage:50 mg/kg
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Administration:p.o.; twice daily; 7 days
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Result:Resulted in time-dependent accumulation of LC3-II in tumor tissue, consistent with reduced autophagic capacity.
Showed no reduction in tumor volume over the 7-day treatment period.
Chemical Information
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CAS No. 1383716-46-8
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Appearance Solid
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분자량 391.47
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화학식 C21H25N7O
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Color White to off-white
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SMILES
CC(O)(C)CNC1=NC=C(C2=NC(NC3=CC=NC=C3)=NC=C2)C(CC4CC4)=N1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 78 mg/mL (199.25 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (279 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5545 mL | 12.7724 mL | 25.5447 mL | 63.8619 mL |
| 5 mM | 0.5109 mL | 2.5545 mL | 5.1089 mL | 12.7724 mL | |
| 10 mM | 0.2554 mL | 1.2772 mL | 2.5545 mL | 6.3862 mL | |
| 15 mM | 0.1703 mL | 0.8515 mL | 1.7030 mL | 4.2575 mL | |
| 20 mM | 0.1277 mL | 0.6386 mL | 1.2772 mL | 3.1931 mL | |
| 25 mM | 0.1022 mL | 0.5109 mL | 1.0218 mL | 2.5545 mL | |
| 30 mM | 0.0851 mL | 0.4257 mL | 0.8515 mL | 2.1287 mL | |
| 40 mM | 0.0639 mL | 0.3193 mL | 0.6386 mL | 1.5965 mL | |
| 50 mM | 0.0511 mL | 0.2554 mL | 0.5109 mL | 1.2772 mL | |
| 60 mM | 0.0426 mL | 0.2129 mL | 0.4257 mL | 1.0644 mL | |
| 80 mM | 0.0319 mL | 0.1597 mL | 0.3193 mL | 0.7983 mL | |
| 100 mM | 0.0255 mL | 0.1277 mL | 0.2554 mL | 0.6386 mL |
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