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BVT948

Catalog No. T14841   CAS 39674-97-0

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

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BVT948 Chemical Structure
BVT948, CAS 39674-97-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 41.00
5 mg In stock $ 96.00
10 mg In stock $ 142.00
25 mg In stock $ 238.00
50 mg In stock $ 353.00
100 mg In stock $ 526.00
1 mL * 10 mM (in DMSO) In stock $ 97.00
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Purity: 98.70%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description BVT948 is a protein tyrosine phosphatase (PTP) inhibitor.It can also inhibit lysine methyltransferase SETD8 (KMT5A) and several cytochrome P450 (P450) isoforms.
In vitro BVT948 exhibits dose-dependent inhibition of TPA-induced MMP-9 up-regulation, without affecting MAPK phosphorylation caused by TPA. It reduces TPA-induced cell invasion by 50%. Interestingly, BVT948 does not significantly alter cell viability in MCF-7 cells at concentrations of 0.5, 1, or 5 μM over 24 hours. Furthermore, BVT948 is a potent inhibitor of protein tyrosine phosphatases (PTP) and P450 activities, demonstrating its ability to selectively suppress H4 lysine 20 (H4K20me1) methylation at doses below 5 μM within 24 hours. Additionally, it enhances the insulin signal's strength without affecting its duration and induces cell-cycle-arrest phenotypes reminiscent of those observed with SETD8 knockdown via RNAi. BVT948 also effectively inhibits TPA-induced NF-κB binding activity but not AP-1 binding activity, showcasing its selective inhibitory properties on specific molecular targets.
In vivo Compare with vehicle-treated controls, BVT948 (BVT.948, 3 μmol/kg) significantly enhances glucose clearance from the blood stream in response to insulin[1].
Molecular Weight 241.24
Formula C14H11NO3
CAS No. 39674-97-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (414.52 mM), Sonication is recommended.

TargetMolReferences and Literature

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.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library ReFRAME Related Library Reprogramming Compound Library Anti-Metabolism Disease Compound Library Histone Modification Compound Library Glycometabolism Compound Library Methylation Compound Library Metabolism Compound Library Anti-Cancer Compound Library Bioactive Compound Library

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Keywords

BVT948 39674-97-0 Chromatin/Epigenetic Metabolism P450 Phosphatase Histone Methyltransferase Cytochrome P450 Inhibitor BVT 948 BVT-948 CYPs inhibit inhibitor

 

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