中文同义词:
G蛋白偶联RHO GEFS抑制剂(Y16);化合物Y16
英文同义词:
Y16;4-[[3-[(3-Methylphenyl)methoxy]phenyl]methylene]-1-phenyl-3,5-pyrazolidinedione;Y16, >98%;Y16, 429653-73-6;3,5-Pyrazolidinedione, 4-[[3-[(3-methylphenyl)methoxy]phenyl]methylene]-1-phenyl-
密度
1.273±0.06 g/cm3(Predicted)
溶解度
DMSO: soluble5mg/mL, clear (warmed)
酸度系数(pKa)
8.84±0.20(Predicted)
颜色
, faint yellow to dark orange
生物活性
Y16是G蛋白偶联Rho GEFs抑制剂。它能阻止LARG和Rho的结合,Kd值为80 nM。
靶点
Target Value
RhoGEFs
()
体外研究
Y16 (10-30 μΜ; 24 hours; NIH 3T3 cells) could inhibit RhoA-GTP formation induced by serum dose dependently and is specific for RhoA.
Y16 (10-30 μΜ; 24 hours; NIH 3T3 cells) efficiently inhibits serum or SDF-1α-induced phospho-MLC and phospho-FAK formation, which are downstream of RhoA.
Cell Viability Assay
Cell Line: NIH 3T3 cells
Concentration: 10 μΜ, 30 μΜ
Incubation Time: 24 hours
Result: Inhibited RhoA-GTP formation induced by serum dose dependently and was specific for RhoA.
Western Blot Analysis
Cell Line: NIH 3T3 cells
Concentration: 10 μΜ, 30 μΜ
Incubation Time: 24 hours
Result: Inhibited serum or SDF-1α-induced phospho-MLC and phospho-FAK formation, which were downstream of RhoA.
Concentration:
10 μΜ, 30 μΜ
Result:
Inhibited RhoA-GTP formation induced by serum dose dependently and was specific for RhoA.
Concentration:
10 μΜ, 30 μΜ
Result:
Inhibited serum or SDF-1α-induced phospho-MLC and phospho-FAK formation, which were downstream of RhoA.
危险品运输编号
UN 3077 9 / PGIII