Vps34-IN-2
Based on 6 publication(s) in Google Scholar
Vps34-IN-2 is a novel, potent and selective inhibitor of Vps34 with IC50s of 2 and 82 nM on the Vps34 enzymatic assay and the GFP-FYVE cellular assay, respectively. Vps34-IN-2 shows antiviral activity against SARS-CoV-2 (IC50 of 3.1 μM), HCoV-229E (IC50 of 0.7 μM) and HCoV-OC43.
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- 純度: 99.73%
- CAS 番号: 1523404-29-6
- 分子式: C18H25F3N4O3
- 分子量:402.41
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保管条件: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]
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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
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Vps34-IN-2
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Customer Validation & Images
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Cell Proliferation/Viability Assay
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IF
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RT-PCR
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
生物活性
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Vps34 2 nM (IC50) |
SARS-CoV-2 3.1 μM (IC50) |
HCoV-229E 0.7 μM (IC50) |
Vps34-IN-2 (Compound 31) displays IC50s of 2 and 82 nM on the Vps34 enzymatic assay and the GFP-FYVE cellular assay, respectively. Vps34-IN-2 exhibits selectivity against mTOR (IC50>10 μM) and class I PI3Ks (IC50 values of 2.7, 4.5, 2.5, and >10 μM on PI3K α, β, δ, γ isoforms, respectively)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1523404-29-6
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性状 Solid
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分子量 402.41
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分子式 C18H25F3N4O3
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Color White to off-white
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SMILES
O=C1C=C(N2[C@H](C)COCC2)N=C3N(CC(C(C)C)=O)[C@H](C(F)(F)F)CCN31
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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 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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Immunity
Alcaligenes faecalis induces intestinal T helper-17 cells by enhancing Rorc transcription through E3 ligase Trim21-mediated Fbxw7 degradation. [Abstract]2025 Apr 8:S1074-7613(25)00128-1. PMID: 40215968 -
Nat Genet
Genome-wide CRISPR screening identifies TMEM106B as a proviral host factor for SARS-CoV-2. [Abstract]2021 Apr;53(4):435-444. PMID: 33686287
Vps34-IN-2 purchased from MedChemExpress. Usage Cited in: Nat Genet. 2021 Apr;53(4):435-444. [Abstract]
eGFP-expressing Vero E6 cells pretreated for 24 h with indicated compounds and infected with SARS-CoV-2. Cell viability without virus was determined by MTS assay 4 d after compound treatment. Cell viability with virus was calculated by measuring the number of eGFP-positive cells compared with uninfected, untreated controls (n = 2 wells from one of two independent experiments with similar results).
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Nat Chem Biol
2025 May 26. PMID: 40419770 -
Vps34-IN-2 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-2 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-2 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-2 was 0.57, 1.80, 0.83, and 0.36 μM against WT, Beta, Delta, and Omicron variants, respectively.
Vps34-IN-2 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 of VPS34-IN-2 was 54.53 μM.
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J Virol
Inhibition of Autophagy Suppresses SARS-CoV-2 Replication and Ameliorates Pneumonia in hACE2 Transgenic Mice and Xenografted Human Lung Tissues. [Abstract]2021 Nov 23;95(24):e0153721. PMID: 34550769 -
Res Sq
2025 Feb 11:rs.3.rs-4138879. PMID: 39989975
溶剤 & 溶解度
Ethanol : 50 mg/mL (124.25 mM; Need ultrasonic)
DMSO : ≥ 50 mg/mL (124.25 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.21 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 EtOH 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% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.21 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 EtOH 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.
Add each solvent one by one: 10% EtOH 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.21 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 EtOH stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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.
プロトコル
Cells are cultured in RPMI-1640 medium with 10% fetal bovine serum. Cells are lysed by sonication in a detergent containing lysis buffer and cleared by centrifugation, and the resulting supernatant is collected for compound treatment. Final protein concentration of lysates is 4 mg/mL. An amount of 5 μL of Vps34-IN-2 (Compound 31) is added from 100× stock solutions in DMSO to 445 μL of lysate in duplicate. An amount of 5 μL of DMSO is added to 445 μL of lysate in quadruplicate for controls. After 15 min incubation, 5 μL of a 100× aqueous solution of the ATP probe I is added to each sample (final concentration of ATP probe I is 0.5 μM). After 5 min, 50 μL of a 10× aqueous solution of the ATP probe II is added to each sample (final concentration of ATP probe II is 20 μM). All samples are then incubated for an additional 10 min[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
For PK/PD studies, 3×106 H1299-GFP-FYVE tumor cells with 50% Matrigel are subcutaneously injected on the dorsal side of SCID mice, one tumor per mouse. When xenografted tumors reach a range of ~200 to 400 mm3, mice are treated with vehicle (98% PEG200/2% PS80) or a single dose of Vps34-IN-2 (compound 31) at 100 and 50 mg/kg via oral gavage. Three mice treated with vehicle alone and three mice treated with Vps34-IN-2 are sacrificed at each time point; tumor tissues are harvested for immunohistochemistry (IHC) analysis and plasma samples are collected to determine the concentration of Vps34-IN-2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (282 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Pasquier B, et al. Discovery of (2S)-8-[(3R)-3-methylmorpholin-4-yl]-1-(3-methyl-2-oxobutyl)-2-(trifluoromethyl)-3,4-dihydro-2H-pyrimido[1,2-a]pyrimidin-6-one: a novel potent and selective inhibitor of Vps34 for the treatment of solid tumors. J Med Chem. 2015 Jan 8;58(1):376-400. [Content Brief]
[2]. Jim Baggen, et al. Genome-wide CRISPR screening identifies TMEM106B as a proviral host factor for SARS-CoV-2. Nat Genet. 2021 Mar 8. [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 |
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| Ethanol / DMSO | 1 mM | 2.4850 mL | 12.4251 mL | 24.8503 mL | 62.1257 mL |
| 5 mM | 0.4970 mL | 2.4850 mL | 4.9701 mL | 12.4251 mL | |
| 10 mM | 0.2485 mL | 1.2425 mL | 2.4850 mL | 6.2126 mL | |
| 15 mM | 0.1657 mL | 0.8283 mL | 1.6567 mL | 4.1417 mL | |
| 20 mM | 0.1243 mL | 0.6213 mL | 1.2425 mL | 3.1063 mL | |
| 25 mM | 0.0994 mL | 0.4970 mL | 0.9940 mL | 2.4850 mL | |
| 30 mM | 0.0828 mL | 0.4142 mL | 0.8283 mL | 2.0709 mL | |
| 40 mM | 0.0621 mL | 0.3106 mL | 0.6213 mL | 1.5531 mL | |
| 50 mM | 0.0497 mL | 0.2485 mL | 0.4970 mL | 1.2425 mL | |
| 60 mM | 0.0414 mL | 0.2071 mL | 0.4142 mL | 1.0354 mL | |
| 80 mM | 0.0311 mL | 0.1553 mL | 0.3106 mL | 0.7766 mL | |
| 100 mM | 0.0249 mL | 0.1243 mL | 0.2485 mL | 0.6213 mL |
Vps34-IN-2 関連分類
HY-12473 関連分類
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