BMS-P5 free base is a specific and orally active peptidylarginine deiminase 4 (PAD4) inhibitor. BMS-P5 free base blocks MM-induced NET formation and delays progression of MM in a syngeneic mouse model.
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.
分子式
C27H32N6O2
分子量
472.58
CAS号
1550371-22-6
运输条件
Room temperature in continental US; may vary elsewhere.