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BVT948 (BVT-948) is a novel and potent protein tyrosine phosphatases (PTP) inhibitor with IC50 of 0.09 - 1.7 μM. Also inhibit several cytochrome P450 (P450) isoforms and lysine methyltransferase SETD8.
| ln Vitro |
The findings show that BVT948 (BVT.948) has no effect on signal duration and instead acts to improve insulin signaling. PTP activity and P450 activity show that BVT948 is a strong kinase of these two protein tyrosine phosphatases [1]. H4 lysine 20 (H4K20me1) is potently and rapidly inhibited by BVT948 over a 24-hour period at doses less than 5 μM. According to reports, cells treated with BVT948 recovered a cell cycle whipping phenotype, which is comparable to SETD8 knockdown via RNA interference [2]. MCF-7 cells treated with 0.5, 1, or 5 μM BVT948 did not exhibit significant changes in viability after a 24-hour incubation period. In a dose-dependent manner, BVT948 prevents MMP-9 upregulation brought on by TPA. TPA-stimulated NF-κB binding activity was inhibited by BVT948 treatment, but not AP-1 binding activity. TPA's phosphorylation of MAPK is unaffected by BVT948. 50% less TPA-induced cellular myocardium was present after BVT948 treatment [3].
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| ln Vivo |
Comparing destination-treated hydrogen with 3 μMol/kg BVT948 (BVT.948) dramatically increased insulin's ability to remove glucose from the circulation [1].
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| References |
[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.
[2]. Blum G, et al. Small-molecule inhibitors of SETD8 with cellular activity. ACS Chem Biol. 2014 Nov 21;9(11):2471-8. [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 |
| Molecular Formula |
C14H11NO3
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|---|---|
| Molecular Weight |
241.24
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| Exact Mass |
241.0739
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| CAS # |
39674-97-0
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| Related CAS # |
39674-97-0;
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| SMILES |
O=C1C(O)=C2C(C3=C1C=CC=C3)=NC(C2(C)C)=O
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| Synonyms |
BVT 948 BVT-948 BVT948
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~414.52 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.62 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (8.62 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.4145 mL | 2.0726 mL | 4.1452 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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