NSC 207895
發(fā)布者：信康 瀏覽次數(shù)：
產(chǎn)品名稱:NSC 207895CAS:58131-57-0別名：4-(4-甲基-1-哌嗪基)-7-硝基-2,1,3-苯并二唑3-氧化物英文名：NSC 207895
- 生物活性NSC 207895抑制MDMX，IC50為2.5 μM，促進(jìn)p53穩(wěn)定/激活和DNA損傷，也調(diào)節(jié)MDM2（E3連接酶）。
- 體外研究NSC-207895 decreases both the MDMX mRNA and protein in MCF-7 cells. NSC-207895 induces expression of p53 as well as well-characterized p53-target gene, p21 and MDM2, in a dose-dependent manner in MCF-7 cells. NSC-207895 extends the half-life of p53 from 20 to 30 minutes to more than 3 hours as revealed by cycloheximide chase assays in MCF-7 cells. NSC-207895 also activates p53 and induces p21 and MDM2 expression in LNCaP prostate and A549 lung cancer cells. NSC-207895 increases the mRNA levels of proapoptotic genes including PUMA, BAX, and PIG3 in a dose-dependent manner in MCF-7 cells. NSC-207895 results in a significant increase in the numbers of sub-G0/G1 cells as well as G2 arrest. NSC-207895 also results in more than 40% of cells dying via apoptosis and decreases cell viability in A549 and LNCaP cells. NSC-207895 inhibits biosynthesis of nucleic acids and proteins in L1210 cells. NSC-207895 interacts with DNA repair to activate the DNA damage repair pathway in three species (S. cerevisiae, S. pombe and H. sapiens). NSC-207895 acts as cytotoxic agent in the G/R-luc astrocytoma cell line with GI50 of 117 nM.
