| Name | BVT948 |
| Description | BVT948 is a protein tyrosine phosphatase (PTP) inhibitor that also inhibits lysine methyltransferase SETD8 (KMT5A) and various 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]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (16.58 mM), Sonication is recommended.
DMSO : 100 mg/mL (414.52 mM), Sonication is recommended.
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| Keywords | SETD8 | PTP | protein tyrosine phosphatase(PTP) | Phosphatase | P450 | Inhibitor | inhibit | HistoneMethyltransferase | Histone Methyltransferase | Cytochrome P450 | CYPs | BVT-948 | BVT948 | BVT 948 |
| Inhibitors Related | Oxadiazon | Musk ketone | Naringin dihydrochalcone | Ipriflavone | Benzyl alcohol | Hexane-1,6-diol | Sudan IV | Stearic acid | Naringin | L-Ascorbic acid 2-phosphate magnesium | Chlorzoxazone | Dibenzothiophene |
| Related Compound Libraries | Histone Modification Compound Library | Reprogramming Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Epigenetics Compound Library | Inhibitor Library | Metabolism Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Metabolism Disease Compound Library | Phosphatase Inhibitor Library |
United States
