BVT948
Based on 2 publication(s) in Google Scholar
BVT948 is a protein tyrosine phosphatase (PTP) inhibitor which can also inhibit several cytochrome P450 (P450) isoforms and lysine methyltransferase SETD8 (KMT5A).
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- Pureza: 98.11%
- No. CAS: 39674-97-0
- Fòrmula: C14H11NO3
- Peso molecular:241.24
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Almacenamiento:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Chemical Information
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Solvente y solubilidad
- Protocolo
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Publications Citing Use of MedChemExpress (MCE) BVT948
MoreVer todos los productos específicos de isoformas Histone Methyltransferase
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Actividad biológica
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SETD8/KMT5A |
Results show that the effect of BVT948 (BVT.948) is to strengthen the insulin signal and has no effects on the duration of the signal. BVT948 appears to be an effective inhibitor of both protein tyrosine phosphatases (PTP activity and P450 activity)[1]. BVT948 efficiently and selectively suppresses cellular H4 lysine 20 (H4K20me1) at doses lower than 5 μM within 24 h. The cells treated with BVT948 recapitulate cell-cycle-arrest phenotypes similar to what are reported for knocking down SETD8 by RNAi[2]. Treatment of MCF-7 cells with 0.5, 1 or 5 μM of BVT948 for 24 h does not cause any significant changes in cell viability.? BVT948 inhibits TPA-induced MMP-9 up-regulation in a dose-dependent manner. Treatment with BVT948 inhibits TPA-stimulated NF-κB binding activity, but not AP-1 binding activity. BVT948 does not affect the MAPK phosphorylation by TPA. Treatment with BVT948 diminishes the TPA-induced cell invasion by 50%[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 39674-97-0
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Appearance Solid
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Peso molecular 241.24
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Fòrmula C14H11NO3
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Color Pink to red
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SMILES
O=C1C(O)=C2C(C3=C1C=CC=C3)=NC(C2(C)C)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
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Journal Impact Factor
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Most Recent
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Int J Parasitol Drugs Drug Resist
The phosphatase inhibitor BVT-948 can be used to efficiently screen functional sexual development proteins in the malaria parasite Plasmodium berghei. [Abstract]2024 Dec:26:100563. PMID: 39153438 -
Int J Parasitol Drugs Drug Resist
Phosphatase inhibitors BVT-948 and alexidine dihydrochloride inhibit sexual development of the malaria parasite Plasmodium berghei. [Abstract]2022 Aug;19:81-88. PMID: 35792443
Solvente y solubilidad
DMSO : 100 mg/mL (414.52 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
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: ≥ 2.08 mg/mL (8.62 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (8.62 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Protocolo
To determine the reversibility of the inhibition of protein tyrosine phosphatases (PTP) activity by BVT948 (BVT.948), 50 ng of PTP1B is incubated in 100 μL of assay buffer with 20 μM BVT948 for 10 min in a concentration device. The sample is then centrifuged at 14,000 rpm at 4°C for 12 min. The concentrate is subsequently washed three times with 100 μL of assay buffer followed by centrifugation. After washing, 190 μL of assay buffer is added to the sample, increasing the volume to 200 μL. Twenty microliters are used in assays measuring enzyme activity remaining using para-nitrophenyl phosphate (pNPP) as a substrate. Controls includes enzyme, which is treated with inhibitor but not washed, and enzyme, which is not treated with BVT948 but is put through the incubation and washing procedures[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
L6 myocytes are maintained in minimum essential medium-alpha (α-MEM) supplemented with 10% fetal bovine serum and 100 IU/mL penicillin-streptomycin at 37°C in 5% CO2. Cells are seeded into 24-well plates, and the medium is replaced with α-MEM containing 2% fetal calf serum to induce differentiation into myotubes. The medium is changed every other day, and cytidine (0.24 mg/mL medium) is added to the cultures at days 7 to 9 to suspend cycling cells. The cells are used in experiments after overnight serum starvation at days 11 to 16. They are treated with or without 25 μM BVT948 (BVT.948) for 30 min followed by 5 min of insulin (25 nM) stimulation. After freezing with liquid N2, the cells are lysed with a Tris-HCl buffer, pH 7.4, containing 1% Nonidet-40, 0.25% sodium deoxycholate, 150 mM NaCl, 1 mM EDTA, 1 mM EGTA, 1 mM sodium orthovanadate, 10 mM β-glycerophosphate, 5 mM sodium pyrophosphate, and complete protease inhibitor cocktail The cell extracts are centrifuged at 14,000 g for 10 min, and the supernatants are used in the Delfia assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Male mice 12 to 14 weeks old are used in this study. They are divided into equal groups (n=9) based on blood glucose levels. At time 0, the mice are injected with vehicle (NaCl with 10% DMSO) or BVT948 (BVT.948) (0.3 and 3 μmol/kg) and 1 U/kg insulin intraperitoneally. Blood glucose is determined from tail vein sampling at 0, 30, 60, and 120 min using a glucometer[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (287 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Liljebris C, et al. Oxidation of protein tyrosine phosphatases as a pharmaceutical mechanism of action: a study using 4-hydroxy-3,3-dimethyl-2H-benzo[g]indole-2,5(3H)-dione. J Pharmacol Exp Ther. 2004 May;309(2):711-9. [Content Brief]
[2]. Blum G, et al. Small-molecule inhibitors of SETD8 with cellular activity. ACS Chem Biol. 2014 Nov 21;9(11):2471-8. [Content Brief]
[3]. Hwang BM, et al. Protein tyrosine phosphatase controls breast cancer invasion through the expression of matrix metalloproteinase-9. BMB Rep. 2013 Nov;46(11):533-8. [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, 6 months; -20°C, 1 month (sealed storage, away from moisture). 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 | 4.1452 mL | 20.7262 mL | 41.4525 mL | 103.6312 mL |
| 5 mM | 0.8290 mL | 4.1452 mL | 8.2905 mL | 20.7262 mL | |
| 10 mM | 0.4145 mL | 2.0726 mL | 4.1452 mL | 10.3631 mL | |
| 15 mM | 0.2763 mL | 1.3817 mL | 2.7635 mL | 6.9087 mL | |
| 20 mM | 0.2073 mL | 1.0363 mL | 2.0726 mL | 5.1816 mL | |
| 25 mM | 0.1658 mL | 0.8290 mL | 1.6581 mL | 4.1452 mL | |
| 30 mM | 0.1382 mL | 0.6909 mL | 1.3817 mL | 3.4544 mL | |
| 40 mM | 0.1036 mL | 0.5182 mL | 1.0363 mL | 2.5908 mL | |
| 50 mM | 0.0829 mL | 0.4145 mL | 0.8290 mL | 2.0726 mL | |
| 60 mM | 0.0691 mL | 0.3454 mL | 0.6909 mL | 1.7272 mL | |
| 80 mM | 0.0518 mL | 0.2591 mL | 0.5182 mL | 1.2954 mL | |
| 100 mM | 0.0415 mL | 0.2073 mL | 0.4145 mL | 1.0363 mL |
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