1. Metabolic Enzyme/Protease Epigenetics
  2. Phosphatase Cytochrome P450 Histone Methyltransferase
  3. BVT948

BVT948 is a protein tyrosine phosphatase (PTP) inhibitor which can also inhibit several cytochrome P450 (P450) isoforms and lysine methyltransferase SETD8 (KMT5A).

For research use only. We do not sell to patients.

BVT948 Chemical Structure

BVT948 Chemical Structure

CAS No. : 39674-97-0

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 99 In-stock
Solution
10 mM * 1 mL in DMSO USD 99 In-stock
Solid
5 mg USD 90 In-stock
10 mg USD 130 In-stock
50 mg USD 270 In-stock
100 mg USD 430 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

BVT948 is a protein tyrosine phosphatase (PTP) inhibitor which can also inhibit several cytochrome P450 (P450) isoforms and lysine methyltransferase SETD8 (KMT5A).

IC50 & Target

PTP[1], P450[1], SETD8[2]

In Vitro

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.

In Vivo

Results show that 3 μmol/kg BVT948 (BVT.948) significantly enhances glucose clearance from the blood stream in response to insulin compare with vehicle-treated controls[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

241.24

Formula

C14H11NO3

CAS No.
Appearance

Solid

Color

Pink to red

SMILES

O=C1C(O)=C2C(C3=C1C=CC=C3)=NC(C2(C)C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.1452 mL 20.7262 mL 41.4525 mL
5 mM 0.8290 mL 4.1452 mL 8.2905 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: ≥99.0%

References
Kinase Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 (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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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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