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。
| Cas No. | 1550371-22-6 |
| Canonical SMILES | CN1C(C2=CC3=CC=CN=C3N2CC4CC4)=NC5=CC(C(N6[C@H](CC[C@H](C6)N)C)=O)=CC(OC)=C15 |
| 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 |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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) |
