BVT 948

BVT 948 is a noncompetitive, cell-permeable inhibitor of protein tyrosine phosphatases (PTP; IC₅₀s = 0.09-1.7 µM).¹ It facilitates the oxidation of the catalytic cysteine residue by hydrogen peroxide.¹ Similarly, it inhibits redox-sensitive cytochrome P450 (CYP) isoforms, including CYP2C19 and CYP2D6, with IC₅₀ values less than 10 µM.¹ BVT 948 also inhibits the protein methyltransferases SETD8, SETD2, G9a, SMYD2, CARM1, and PRMT3 with IC₅₀ values from 0.7 to 3.2 µm.² Presumably through its effects on PTPs, BVT 948 enhances insulin signaling in cells and insulin tolerance in ob/ob mice, suppresses the expression of matrix metalloproteinase-9 and invasion in breast cancer cells, and increases NMDA-induced substance P release by spinal cord slices.^1,3,4

WARNING This product is not for human or veterinary use.

1. Liljebris, C., Baranczewski, P., Björkstrand, E., 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. 309(2), 711-719 (2004).

2. Blum, G., Ibáñez, G., Rao, X., et al. Small-molecule inhibitors of SETD8 with cellular activity. ACS Chem. Biol. 9(11), 2471-2478 (2014).

3. Hwang, B.M., Chae, H.S., Jeong, Y.J., et al. Protein tyrosine phosphatase controls breast cancer invasion through the expression of matrix metalloproteinase-9. BMB Rep. 46(11), 533-538 (2013).

4. Chen, W., Zhang, G., and Marvizón, J.C.G. NMDA receptors in primary afferents require phosphorylation by Src family kinases to induce substance P release in the rat spinal cord. Neuroscience 166(3), 924-934 (2010).