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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 98.79%
- CAS 番号: 1383716-46-8
- 分子式: C21H25N7O
- 分子量:391.47
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保管条件: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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
製品説明
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 |
体外実験
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
体内実験
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.
化学情報
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CAS 番号 1383716-46-8
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性状 Solid
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分子量 391.47
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
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 |
Vps34-IN-4 関連分類
HY-123058 関連分類
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