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逆转素(Reversine)

腺苷受体、非肌肉肌球蛋白 II (NM II)、MEK1 和极光激酶抑制剂

产品号 #(选择产品)

产品号 #72612_C

腺苷受体、非肌肉肌球蛋白 II (NM II)、MEK1 和极光激酶抑制剂

总览

逆转素(Reversine)是一种 2,6-二取代的嘌呤衍生物,可抑制人类 A3 腺苷受体、非肌肉肌球蛋白 II 重链、丝裂原激活的细胞外信号调节激酶-1 (MEK1) 和 Aurora B 激酶 (Chen et al.; Perreira et al.; D’Alise et al.)。

重编程
·诱导小鼠成肌细胞去分化为具有成骨和脂肪潜能的多能祖细胞(Chen et al., 2007; Chen et al., 2004)。
·诱导小鼠和人原代真皮成纤维细胞去分化为具有成肌能力的细胞 (Anastasia et al.)。
·诱导纤维环细胞去分化为具有向软骨形成、成骨形成或脂肪形成谱系发育潜力的多能间充质祖细胞(Saraiya et al.)。

癌症研究
·在PC-3、HeLa、CWR22Rv1和DU-145癌细胞系中抑制细胞增殖并诱导多倍体(Hsieh et al.)。
·诱导人胚胎癌细胞系 NT2 和人早幼粒细胞白血病细胞系 HL60 的分化(D’Alise et al.)。
·抑制多种癌细胞系的增殖、导致胞质分裂失败并诱导多倍体化(D’Alise et al.)。

细胞类型
癌细胞及细胞系,白血病/淋巴瘤细胞,间充质干/祖细胞,肌源干/祖细胞
 
种属
人,小鼠,非人灵长类,其它细胞系,大鼠
 
应用
重编程
 
研究领域
癌症,干细胞生物学
 
CAS 编号
656820-32-5
 
化学式
C₂₁H₂₇N₇O
 
纯度
> 95%
 
通路
腺苷,极光激酶,MEK/ERK
 
靶点
腺苷受体,极光激酶B,MEK1,NM II
 

产品说明书及文档

请在《产品说明书》中查找相关支持信息和使用说明,或浏览下方更多实验方案。

Document Type
Product Name
Catalog #
Lot #
Language
Product Name
Reversine
Catalog #
72614, 72612
Lot #
For 72612 lot 1000098536 and higher | For 72614 lot 1000092114 and higher
Language
English
Document Type
Safety Data Sheet
Product Name
Reversine
Catalog #
72614, 72612
Lot #
All
Language
English

应用领域

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相关材料与文献

技术资料 (3)

文献 (7)

Reversine enhances generation of progenitor-like cells by dedifferentiation of annulus fibrosus cells. Saraiya M et al. Tissue engineering. Part A 2010 APR

Abstract

The aim of this study was to determine if treatment with reversine, a purine analog, promoted generation of skeletal progenitor cells from lineage-committed annulus fibrosus cells. Reversine modulated cell growth, morphology, and the actin cytoskeleton of annulus fibrosus cells. Microarray profiling coupled with Ingenuity Pathway Analysis revealed that reversine treatment resulted in a significant expression change in many genes including those required for cell-cell interaction, cell movement, cell growth, and development. Further analysis revealed that there was involvement of gene networks concerned with cellular assembly and organization, DNA replication and repair, tissue morphology, and cell-to-cell signaling. The gene expression profile was dependent on reversine concentration. In osteogenic media, cells pretreated with 300 nM reversine exhibited an increased induction in alkaline phosphatase activity and enhanced expression of alkaline phosphatase, bone sialoprotein, osteocalcin, and collagen type I mRNA. Maintained in adipogenic media, the reversine-pretreated annulus cells displayed evidence of adipogenic differentiation: accumulation of cytosolic lipid droplets and increased expression of PPAR-gamma2, LPL, and Fabp mRNA. In chondrogenic media, cells pretreated with reversine exhibited marked increase in the induction of aggrecan, collagen types II, IX, and XI, and versican. It is concluded that reversine treatment induced annulus fibrosus cell plasticity and promoted their differentiation along mesenchymal lineages. This agent could be used to generate skeletal progenitor cells to orchestrate the repair of the intervertebral disc.
Reversine, a novel Aurora kinases inhibitor, inhibits colony formation of human acute myeloid leukemia cells. D'Alise AM et al. Molecular cancer therapeutics 2008 MAY

Abstract

The demonstration that the small synthetic molecule reversine [2-(4-morpholinoanilino)-N6-cyclohexyladenine] promotes the dedifferentiation of committed cells into multipotent progenitor-type cells has raised hopes on the exploitation of this small chemical tool for the generation of stem cells. Here, we show that reversine causes a failure in cytokinesis and induces polyploidization. These effects of reversine are due to the inhibition of Aurora A and B, two related kinases that are implicated in several aspects of mitosis and that are frequently amplified and overexpressed in human tumors. Reversine inhibits the phosphorylation of histone H3, a direct downstream target of Aurora kinases. Similarly to the Aurora kinase inhibitor VX-680, which has recently entered phase II clinical trials for cancer treatment, reversine inhibited colony formation of leukemic cells from patients with acute myeloid leukemia but was significantly less toxic than VX-680 on cells from healthy donors. The crystal structure of the reversine-Aurora B kinase complex shows that reversine is a novel class of ATP-competitive Aurora kinase inhibitors. Thus, although our studies raise serious doubts on the application of reversine in regenerative medicine, they support the paradigm that reversine might be a useful agent in cancer chemotherapy.
Reversine increases the plasticity of lineage-committed mammalian cells. Chen S et al. Proceedings of the National Academy of Sciences of the United States of America 2007 JUN

Abstract

Previously, a small molecule, reversine, was identified that reverses lineage-committed murine myoblasts to a more primitive multipotent state. Here, we show that reversine can increase the plasticity of C2C12 myoblasts at the single-cell level and that reversine-treated cells gain the ability to differentiate into osteoblasts and adipocytes under lineage-specific inducing conditions. Moreover, reversine is active in multiple cell types, including 3T3E1 osteoblasts and human primary skeletal myoblasts. Biochemical and cellular experiments suggest that reversine functions as a dual inhibitor of nonmuscle myosin II heavy chain and MEK1, and that both activities are required for reversine's effect. Inhibition of MEK1 and nonmuscle myosin II heavy chain results in altered cell cycle and changes in histone acetylation status, but other factors also may contribute to the activity of reversine, including activation of the PI3K signaling pathway.

更多信息

更多信息
种属 Human, Mouse, Non-Human Primate, Other, Rat
Cas Number 656820-32-5
Chemical Formula C₂₁H₂₇N₇O
纯度 > 95%
Target Adenosine Receptor, Aurora Kinase B, MEK1, NM II
Pathway Adenosine, Aurora Kinase, MEK/ERK
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