A PAD4 inhibitor
BMS-P5 is an inhibitor of protein arginine deiminase 4 (PAD4; IC50 = 0.098 µM).1 It is selective for PAD4 over PAD1, -2, and -3 (IC50s = >10 µM for all). BMS-P5 (1 µM) inhibits citrullination of histone H3 and neutrophil extracellular trap (NET) formation induced by RPMI-8226- or MM.1S-conditioned medium in isolated human neutrophils. It delays disease onset and increases survival in a DP42 syngeneic mouse model of multiple myeloma when administered at a dose of 50 mg/kg.
1.Li, M., Lin, C., Deng, H., et al.A novel peptidylarginine deiminase 4 (PAD4) inhibitor BMS-P5 blocks formation of neutrophil extracellular traps and delays progression of multiple myelomaMol. Cancer Ther.19(7)1530-1538(2020)
动态评分
0.0