产品描述: | BMS-P5 is a specific and orally active peptidylarginine deiminase 4 (PAD4) inhibitor. BMS-P5 blocks MM-induced NET formation and delays progression of MM in a syngeneic mouse model |
靶点: |
PAD |
体外研究: |
BMS-P5 blocks calcium ionophore-induced citrullination of histone H3. BMS-P5 is also able to inhibit formation of NETs induced by primary MM cells isolated from the BM of patients with MM. Cell Viability Assay Cell Line: Neutrophils. Concentration: 10 µM and 100 µM. Incubation Time: 30 min followed by addition of DP42 or 5TGM1 CM. Result: Prevented MM-induced NET formation. |
体内研究: |
BMS-P5 (50 mg/kg, oral gavage) significantly improves survival of MM-bearing mice. BMS-P5 (50 mg/kg, oral gavage) may attenuate the presence of pro-tumorigenic proteins in the tumor microenvironment, and thus delay tumor progression. Animal Model: Syngeneic mouse model of MM. Dosage: 50 mg/kg. Administration: Oral gavage, twice a day beginning on day 3 after tumor cell injection. Result: Significantly delayed development of symptoms and significantly prolonged survival of MM-bearing mice. |
参考文献: |
1. Marina Li, et al. A Novel Peptidylarginine Deiminase 4 (PAD4) Inhibitor BMS-P5 Blocks Formation of Neutrophil Extracellular Traps and Delays Progression of Multiple Myeloma. Mol Cancer Ther. 2020 Jul;19(7):1530-1538. |
溶解性: |
Soluble in DMSO |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
1.964 ml |
9.822 ml |
19.644 ml |
5 mM |
0.393 ml |
1.964 ml |
3.929 ml |
10 mM |
0.196 ml |
0.982 ml |
1.964 ml |
50 mM |
0.039 ml |
0.196 ml |
0.393 ml |
|
注意: |
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