NSC319726是一种突变型 p53R175 再激活剂,可抑制表达 p53R175 突变的成纤维细胞的生长,IC50值为8nM。
产品描述
NSC319726, a mutant p53R175 reactivator, suppresses growth of fibroblasts that expresses the p53R175 mutation (IC50 = 8 nM).
体外活性
在p53(R172H/R172H)小鼠中, NSC319726(5 mg/kg)会产生较强的毒性,存活率低.在TOV112D-p53(R175H) 移植瘤中,NSC319726能够抑制瘤细胞生长.
体内活性
在突变型p53的细胞中,NSC319726(IC50=8 nM)可使突变蛋白发生WT样构象变化,从而修复序列特异性的p53转录。
激酶实验
MTS: 5,000 cells of TOV112D cells (5,000 cells/well, in 100 ml culture) are cultured in 96-well plate to reach the 50%–60% confluence on the second day when treated with serial dilutions of the compounds. The growth is measured by MTS reagent and Victor Plate reader instrument after incubation for 3 days.
细胞实验
Viability assays are done. The cells (5×104 cells/well, in 1 ml culture) are cultured in a 12-well plate to reach the 50%–60% confluence on the second day when treated with serial dilutions of the compound. The growth is measured by Guava ViaCount reagent and Guava PCA instrument after incubation for 3 days.(Only for Reference)
Cas No.
71555-25-4
分子式
C11H14N4S
分子量
234.32
别名
ZMC1
储存和溶解度
Ethanol:2.3 mg/mL (10 mM)),with gentle warming
DMSO:23.4 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years