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BVT-948

  Cat. No.:  DC21685   Featured
Chemical Structure
39674-97-0
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More than 5000 active chemicals with high quality for research!
Field of application
BVT-948 (SPS8I-3) is a noncompetitive, cell-permeable inhibitor of protein tyrosine phosphatases (PTPs) with IC50 of 0.09-1.7 uM. Results show that the effect of BVT948 (BVT.948) is to strengthen the insulin signal and has no effects on the duration of th
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 39674-97-0
Chemical Name: 4-hydroxy-3,3-dimethyl-2H-benz[g]indole-2,5(3H)-dione
Synonyms: SPS8I-3
SMILES: OC1C(=O)C2C=CC=CC=2C2C=1C(C)(C)C(=O)N=2
Formula: C14H11NO3
M.Wt: 241.2
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [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-mole
Description: BVT948 is a protein tyrosine phosphatase (PTP) inhibitor which can also inhibit several cytochrome P450 (P450) isoforms and lysine methyltransferase SETD8.
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].
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].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
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