AZ3146
發(fā)布者：信康 瀏覽次數(shù)：
產(chǎn)品名稱:AZ3146CAS:1124329-14-1別名：9-環(huán)戊基-7,9-二氫-2-[[2-甲氧基-4-[(1-甲基-4-哌啶基)氧基]苯基]氨基]-7-甲基-8H-嘌呤-8-酮;9-環(huán)戊基-2-[[2-甲氧基-4-[(1-甲基哌啶-4-基)氧基]-苯基]氨基]-7-甲基-7,9-二氫-8H-嘌呤-8-酮英文名：9-Cyclopentyl-2-[[2-methoxy-4-[(1-methylpiperidin-4-yl)oxy]-phenyl]amino]-7-methyl-7,9-dihydro-8H-purin-8-one
- 密度 1.279
- 儲存條件 Store at +4°C
- 生物活性AZ 3146是一種選擇性Mps1抑制劑，IC50為35 nM左右，有助于招募CENP-E(驅(qū)動蛋白相關(guān)的動力蛋白)，對FAK， JNK1， JNK2和Kit作用效果稍弱。
- 體外研究AZ3146 also inhibits FAK, JNK1, JNK2 and Kit. AZ3146 significantly inhibits phosphorylation of Mps1 in cells. Mitotic-specific phospho forms of aurora B and BubR1 are not affected by AZ3146. AZ3146 does not inhibit Cdk1 or aurora B in mitotic cells. HeLa cells treated with nocodazole and 2 μM AZ3146 only delay mitosis briefly and then rereplicate their genomes, indicating that AZ3146 overrides the SAC. AZ3146 also inhibits an already established SAC signal, as after release from a nocodazole block, AZ3146 dramatically accelerates mitotic exit.During an otherwise unperturbed mitosis, AZ3146 reduces the time to complete mitosis from 90 minutes in controls to 32 minutes. Strikingly, ~90% of AZ3146-treated HeLa cells undergo abnormal mitoses, although ~50% enter anaphase without aligning all of their chromosomes, and ~30% exit mitosis without undergoing obvious chromosome segregation. AZ3146 has a dramatic effect on kinetochore localization of Mad2, reducing its levels to ~15%, but its effect on Mad1 is less pronounced, with levels remaining at ~60%. When Mps1 is inhibited by AZ3146 before mitotic entry, subsequent recruitment of Mad1 and Mad2 to kinetochores is abolished. However, if Mps1 is inhibited by AZ3146 after mitotic entry, the Mad1–C-Mad2 core complex remains kinetochore bound, but O-Mad2 is not recruited to the core.
