Development of a <i>Vaccinia</i> H1‐Related (VHR) Phosphatase Inhibitor with a Nonacidic Phosphate‐Mimicking Core Structure

Abstract

Phosphate Surrogate: A potent vaccinia H1-related (VHR) phosphatase inhibitor with a nonacidic core structure has been developed. RK-682 enamine (RE) derivatives were found to be dual-specificity protein phosphatases (DSP)-selective and cell-permeable. The most VHR-selective compound, RE12, induced cell-cycle arrest in NIH3T3 cells at G1 phase and inhibited dephosphorylation of VHR substrates, such as phospho-ERK and phospho-JNK.