Reversine
(Synonyms: 逆转素) 目录号 : GC14651
Reversine是一种靶向Aurora A激酶、Aurora B激酶和MPS1（Monopolar Spindle 1）激酶的非特异性、具有口服活性的小分子抑制剂。Reversine常用于细胞分化和多种癌症的研究。
Cas No.:656820-32-5
Sample solution is provided at 25 µL, 10mM.
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Reversine is a non-specific, orally active small molecule inhibitor of Aurora A kinase, Aurora B kinase and MPS1 (Monopolar Spindle 1) kinase. Reversine is often used in the study of cell differentiation and various cancer[1-8].
Reversine (0.5, 1, 5, 10 and 20μM; 72h) inhibits the growth of A549 and H1299 cells and suppresses the colony formation of human non-small cell lung cancer cells[1]. Reversine (1, 2, 4μM; 24h) significantly inhibited the expression of MEK1 protein in human osteosarcoma cell lines MNNG/HOS, U-2 OS and MG-63, thereby targeting MEK1 protein to exert anti-tumor effects[2]. In HL60 cells, Reversine (5-10μM; 72h) significantly increased the number of CD11b+ and induced cell differentiation[3]. Reversine(5μM; 4d) increases the plasticity of long-term cryopreserved fibroblasts to multipotent progenitor cells through activation of Oct4[4]. Reversine((0, 1, 5, 10µM; 24h) induces cell cycle arrest and apoptosis via upregulation of the Fas and DR5 signaling pathways in SW480 and HCT116 cells[5].
In the rat bile duct ligation model of ductal reactivity, Reversine (20mg/kg; every 3 days for 2 weeks; ip) attenuated rat cholestatic ductal reactivity and fibrosis and reduced bile duct formation associated with Dlk1/Notch/Sox9 signaling[6]. In the mice MDA-MB-231 cell xenograft model, Reversine (1.0mg/kg; every 7 days for 3 weeks; po) and miR-21-5p inhibitor synergistically exerted tumor suppressive effects on HBC cells by targeting SPRY2[7]. In the highly metastatic MDA231-M2 Orthotopic breast cancer mouse models, 10 and 30mg/kg Reversine treatment significantly reduced the mean number of lung surface metastases by 50% and 70%, respectively[8].
References:
[1]. Lu Y C, Lee Y R, Liao J D, et al. Reversine induced multinucleated cells, cell apoptosis and autophagy in human non-small cell lung cancer cells[J]. PloS one, 2016, 11(7): e0158587.
[2]. Chen X, Zhong Y, Wang S, et al. Reversine inhibits proliferation and induces apoptosis of human osteosarcoma cells through targeting MEK1[J]. Journal of Bone Oncology, 2024, 46: 100601.
[3]. D'Alise A M, Amabile G, Iovino M, et al. Reversine, a novel Aurora kinases inhibitor, inhibits colony formation of human acute myeloid leukemia cells[J]. Molecular cancer therapeutics, 2008, 7(5): 1140-1149.
[4]. Li X, Guo Y, Yao Y, et al. Reversine increases the plasticity of long-term cryopreserved fibroblasts to multipotent progenitor cells through activation of Oct4[J]. International Journal of Biological Sciences, 2016, 12(1): 53.
[5]. Park Y L, Ha S Y, Park S Y, et al. Reversine induces cell cycle arrest and apoptosis via upregulation of the Fas and DR5 signaling pathways in human colorectal cancer cells[J]. International journal of oncology, 2019, 54(5): 1875-1883.
[6]. Huang D, Tang L, Li T, et al. Reversine attenuates cholestatic ductular reaction in rats[J]. FEBS Open bio, 2023, 13(5): 898-911.
[7]. Zhang Y, Wang Y, Xue J, et al. Co-treatment with miR-21-5p inhibitor and Aurora kinase inhibitor reversine suppresses breast cancer progression by targeting sprouty RTK signaling antagonist 2[J]. Bioengineered, 2022, 13(1): 455-468.
[8]. Bijian K, Lougheed C, Su J, et al. Targeting focal adhesion turnover in invasive breast cancer cells by the purine derivative reversine[J]. British journal of cancer, 2013, 109(11): 2810-2818.
Reversine是一种靶向Aurora A激酶、Aurora B激酶和MPS1（Monopolar Spindle 1）激酶的非特异性、具有口服活性的小分子抑制剂。Reversine常用于细胞分化和多种癌症的研究[1-8]。
Reversine（0.5、1、5、10、20μM；72h）抑制A549和H1299细胞的生长，并抑制人非小细胞肺癌细胞的集落形成[1]。Reversine 显著抑制人骨肉瘤细胞系MNNG/HOS、U-2 OS和MG-63中MEK1蛋白的表达，从而通过靶向MEK1蛋白发挥抗肿瘤作用[2]。在HL60细胞中，Reversine（5-10μM；72h）显著增加CD11b+细胞数量并诱导细胞分化[3]。Reversine（5μM；4d）通过激活Oct4，增加长期冷冻保存的成纤维细胞向多能祖细胞的可塑性[4]。Reversine（0、1、5、10µM；24h）通过上调Fas和DR5信号通路，诱导SW480和HCT116细胞的细胞周期阻滞和凋亡[5]。
在大鼠胆管结扎模型中，Reversine（20mg/kg；每3天一次，持续2周；ip）减轻了大鼠胆汁淤积性胆管反应性和纤维化，并通过Dlk1/Notch/Sox9信号通路减少胆管形成[6]。在小鼠MDA-MB-231细胞异种移植模型中，Reversine（1.0mg/kg；每周一次，持续3周；po）与miR-21-5p抑制剂协同作用时，可通过靶向SPRY2发挥对HBC细胞的肿瘤抑制作用[7]。在高度转移性MDA231-M2原位乳腺癌小鼠模型中，10和30mg/kg的Reversine治疗分别使肺表面转移的平均数量减少了50%和70%[8]。
| Kinase experiment [1]: | |
Preparation Method | In vitro kinase assay was carried out using human recombinant full-length FAK incubated in kinase buffer containing ATP and the substrate for 4 h at room temperature with or without the presence of Reversine at a final concentration of 1μM. The remaining ATP in solution was then quantified utilising the Kinase-Gloluminescence kit. |
Reaction Conditions | 1μM; 4h |
Applications | Reversine at a concentration of 1μM inhibited the kinase activity of FAK and its homolog Pyk2 by 70% and 82%, respectively. |
| Cell experiment [1]: | |
Cell lines | MDA-MB-231 cells |
Preparation Method | Cells were seeded on LabTek2 multiwell coverslips at approximately 25% confluence and incubated for 24h. Cells were transfected with 1μg of green fluorescent protein-Paxillin using Lipofectamine LTX. Cells were serum starved for 24h and then stimulated with 20ng/ml epidermal growth factor in the presence or absence of 1μM Reversine or 1μM ret Reversine in DMSO. |
Reaction Conditions | 1μM; 24h |
Applications | In Reversine-treated MDA231-M2 cells, the activation of the FAK Y397 autophosphorylation site was decreased in a dose-dependent manner. |
| Animal experiment [1]: | |
Animal models | Orthotopic breast cancer mouse models |
Preparation Method | For primary tumors, MDA-MB-231 cells were implanted subcutaneously into the mammary fat pad of female SCID mice. Three weeks later, mice were injected intraperitoneally with Reversine (DMSO stock solution further diluted in vehicle: PEG-400 (35%), 100% ETOH (10%), 0.9% NaCl (55%)) once every two weeks at a dose of 10 or 30mg/kg for 4 weeks and stopped 1 week before the end of the study. |
Dosage form | 10, 30mg/kg; ip; 4 weeks |
Applications | In the highly metastatic MDA231-M2 model, 10 and 30mg/kg Reversine treatment significantly reduced the mean number of lung surface metastases by 50% and 70%, respectively. |
References: | |
| Cas No. | 656820-32-5 | SDF | |
| 别名 | 逆转素 | ||
| 化学名 | 6-N-cyclohexyl-2-N-(4-morpholin-4-ylphenyl)-7H-purine-2,6-diamine | ||
| Canonical SMILES | C1CCC(CC1)NC2=NC(=NC3=C2NC=N3)NC4=CC=C(C=C4)N5CCOCC5 | ||
| 分子式 | C21H27N7O | 分子量 | 393.49 |
| 溶解度 | ≥ 19.65 mg/mL in DMSO, ≥ 6.69 mg/mL in EtOH with ultrasonic and warming | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5414 mL | 12.7068 mL | 25.4136 mL |
| 5 mM | 0.5083 mL | 2.5414 mL | 5.0827 mL |
| 10 mM | 0.2541 mL | 1.2707 mL | 2.5414 mL |
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