中文同义词:
逆转素;逆转素, >96%;AURORA激酶抑制剂(REVERSINE);N6-环己基-N2-(4-吗啉苯基)-9H-嘌呤-2,6-二胺
英文同义词:
9H-Purine-2,6-diamine,N6-cyclohexyl-N2-[4-(4-morpholinyl)phenyl]-;N6-Cyclohexyl-N2-(4-morpholinophenyl)-7H-purine-2,6-diamine;2-(4-MORPHOLINOANILINO)-6-CYCLOHEXYLAMINOPURINE;N6-CYCLOHEXYL-N2-(4-MORPHOLINOPHENYL)-9H-PURINE-2,6-DIAMINE;Picropodophyllin (PPP);N6-Cyclohexyl-N2-[4-(4-morpholinyl)phenyl]-1H-purine-2,6-diamine Reversine;Reversine N6-Cyclohexyl-N2-[4-(4-morpholinyl)phenyl]-1H-purine-2,6-diamine;REVERSINE
相关类别:
小分子抑制剂;小分子抑制剂，天然产物;细胞生物学试剂;Inhibitors
沸点
736.4±70.0 °C(Predicted)
密度
1.343±0.06 g/cm3(Predicted)
溶解度
DMSO: 7 mg/mL, soluble
酸度系数(pKa)
10.51±0.10(Predicted)
生物活性
Reversine是一种强效human A3 adenosine receptor拮抗剂，Ki为0.66 μM，也是一种泛aurora A/B/C kinase抑制剂，IC50分别为12 nM/13 nM/20 nM。也用于干细胞分化。
体外研究
Reversine induces myogenic lineage-committed cells to become multipotent mesenchymal progenitor cells, which proliferates and redifferentiates into bone and fat cells. Reversine, as an A3 adenosine receptor antagonist, competitively inhibits forskolin-stimulated cAMP production in stably transfected Chinese hamster ovary (CHO) cells. Reversine inhibits the phosphorylation of a well-known Aurora target, histone H3 in HCT116 cells. Moreover, Reversine potently blocks proliferation of multiple tumor cell types, and induces cell death. In primary human tumor samples, Reversine also inhibits colony formation of leukemic cells. When treated in combination, reversine and aspirin synergistically inhibit growth of cervical cancer cells and induce cell apoptosis.
体内研究
In mice inoculated with U14 tumors, Reversine (10 mg/kg i.p.) and aspirin cause more reduced tumor weight and tumor volume when compared with the control agents.
