BMS-P5 是一种特异性且具有口服活性的肽基精氨酸脱亚胺酶 4 (PAD4) 抑制剂。 BMS-P5 在同基因小鼠模型中阻断 MM 诱导的 NET 形成并延缓 MM 的进展。
货号:ajcx24156
CAS:1550371-22-6
分子式:C27H32N6O2
分子量：472.6
溶解度:DMF: 20 mg/ml,DMSO: 5 mg/ml,Ethanol: 30 mg/ml,Ethanol:PBS (pH 7.2) (1:8): 0.11 mg/ml
纯度：98%
存储：Store at -20°C
库存：现货

Background:

BMS-P5 is an inhibitor of protein arginine deiminase 4 (PAD4; IC₅₀= 0.098 µM).¹It 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)