BVT948 is a protein tyrosine phosphatase (PTP) inhibitor that also inhibits lysine methyltransferase SETD8 (KMT5A) and various cytochrome P450 (P450) isoforms.

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.

Compare with vehicle-treated controls, BVT948 (BVT.948, 3 μmol/kg) significantly enhances glucose clearance from the blood stream in response to insulin[1].