| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg | |||
| 100mg | |||
| Other Sizes |
| Targets |
Protein tyrosine phosphatases (PTPs), including PTP1B, TCPTP, SHP-2, LAR, and YopH. BVT948 is a non-competitive, irreversible inhibitor of PTPs. It also inhibits lysine methyltransferase SETD8 (KMT5A) and several cytochrome P450 isoforms.
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| 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].
BVT948 inhibits PTP1B, TCPTP, SHP-2, LAR, and YopH with IC50s of 0.9, 1.7, 0.09, 1.5, and 0.7 μM, respectively. It displays irreversible inhibition through catalysis of the hydrogen peroxide-dependent oxidation of PTP. BVT948 increases tyrosine phosphorylation of cellular proteins, including the insulin receptor. It enhances insulin signaling in vitro. |
| 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].
In vivo, BVT948 enhances insulin tolerance in ob/ob mice and significantly enhances glucose clearance from the bloodstream in response to insulin. It enhances insulin signaling in vitro and insulin tolerance in ob/ob mice in vivo. The compound has been studied for its potential to improve insulin sensitivity. |
| Enzyme Assay |
In vitro enzyme assays for BVT948 involve measuring its inhibition of protein tyrosine phosphatase (PTP) activity. PTP enzymes are incubated with a phosphotyrosine-containing substrate and various concentrations of BVT948. Phosphate release is measured colorimetrically or using fluorescent substrates. IC50 values are determined from concentration-response curves.
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| Cell Assay |
In vitro cellular assays for BVT948 involve treating cells with the compound and measuring protein tyrosine phosphorylation, insulin receptor phosphorylation, or insulin signaling. Cells are treated with various concentrations of BVT948, and protein phosphorylation is assessed by Western blot using phospho-specific antibodies. The compound's ability to enhance insulin signaling is evaluated.
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| Animal Protocol |
In vivo animal studies for BVT948 typically involve administration to rodent models of insulin resistance or diabetes. Glucose tolerance tests and insulin tolerance tests are performed. BVT948 enhances insulin tolerance in ob/ob mice and significantly enhances glucose clearance from the bloodstream in response to insulin.
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| ADME/Pharmacokinetics |
BVT948 has a molecular weight of 241.24 and a molecular formula of C14H11NO3. It is a non-competitive, irreversible, and cell-permeable inhibitor of protein tyrosine phosphatases. The compound also inhibits lysine methyltransferase SETD8 and several cytochrome P450 isoforms.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies of BVT948 are limited. The compound is a non-competitive, irreversible inhibitor of protein tyrosine phosphatases. It enhances insulin signaling and has been studied for its potential to improve insulin sensitivity. Comprehensive toxicological evaluation is needed before clinical development. The compound should be handled with appropriate safety precautions.
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| References |
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| Additional Infomation |
BVT948 is a non-competitive, irreversible, and cell-permeable inhibitor of protein tyrosine phosphatases (PTPs). It inhibits PTP1B, TCPTP, SHP-2, LAR, and YopH with IC50s ranging from 0.09 to 1.7 μM. BVT948 enhances insulin signaling in vitro and insulin tolerance in ob/ob mice in vivo. It also inhibits lysine methyltransferase SETD8 and several cytochrome P450 isoforms. It is a valuable research tool for studying insulin signaling and PTP function.
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| Molecular Formula |
C14H11NO3
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|---|---|
| Molecular Weight |
241.24
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| Exact Mass |
241.074
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| Elemental Analysis |
C, 69.70; H, 4.60; N, 5.81; O, 19.90
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| CAS # |
39674-97-0
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| Related CAS # |
39674-97-0;
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| PubChem CID |
6604934
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| Appearance |
Pink to red solid powder
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| Density |
1.39g/cm3
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| Boiling Point |
400.8ºC at 760 mmHg
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| Flash Point |
196.2ºC
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| Index of Refraction |
1.679
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| LogP |
1.486
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
18
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| Complexity |
501
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1C(O)=C2C(C3=C1C=CC=C3)=NC(C2(C)C)=O
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| InChi Key |
LLPBUXODFQZPFH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H11NO3/c1-14(2)9-10(15-13(14)18)7-5-3-4-6-8(7)11(16)12(9)17/h3-6H,1-2H3,(H,15,18)
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| Chemical Name |
3,3-dimethyl-1H-benzo[g]indole-2,4,5-trione
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| Synonyms |
BVT 948 BVT-948 BVT948
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| HS Tariff Code |
2934.99.03.00
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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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