Reversine

製品コードS7588 バッチS758801

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C21H27N7O
分子量 393.23 CAS No. 656820-32-5
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 5 mg/mL (12.71 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
0.25mg/ml Taking the 1 mL working solution as an example, add 50 μL of 5 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil
0.25mg/ml Taking the 1 mL working solution as an example, add 50 μL of 5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Reversine is a potent human A3 adenosine receptor antagonist with Ki of 0.66 μM, and a pan-aurora A/B/C kinase inhibitor with IC50 of 400 nM/500 nM/400 nM, respectively. Also used for stem cell dedifferentiation.
in vitro Reversine induces myogenic lineage-committed cells to become multipotent mesenchymal progenitor cells, which proliferates and redifferentiates into bone and fat cells. [1] Reversine, as an A3 adenosine receptor antagonist, competitively inhibits forskolin-stimulated cAMP production in stably transfected Chinese hamster ovary (CHO) cells. [2] 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. [3] When treated in combination, reversine and aspirin synergistically inhibit growth of cervical cancer cells and induce cell apoptosis. [4]
in vivo 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. [4]

プロトコル(参考用のみ)

キナーゼアッセイ Radioligand Binding Assays
Each tube in the A3 AR competitive binding assay contains 100 μL of membrane suspension (20 μg of protein), 50 μL of [125I]4-amino-3-iodobenzyl)adenosine-5′-N-methyluronamide (0.5 nM), and 50 μL of increasing concentrations of the test ligands in Tris-HCl buffer (50 mM, pH 7.4) containing 10 mM MgCl2 and 1 mM EDTA. Nonspecific binding is determined using 10 mM 5′-N-ethylcarboxamidoadenosine in the buffer. The mixtures are incubated at 25°C for 60 min. Binding reactions are terminated by filtration through Whatman GF/B filters under reduced pressure using a MT-24 cell harvester. Filters are washed three times with 9 mL of ice-cold buffer. Radioactivity is determined using a Beckman γ-counter, and the percent inhibition is calculated.
細胞アッセイ 細胞株 HL-60, A375, HeLa, HCT-116, T47D, and MCF-7 cell lines
濃度 ~10 μM
反応時間 72 hours
実験の流れ Cell viability of different tumor cell lines is assessed using ATPlite 1step. Briefly, 2 × 104 cells for each well are plated in a 96-well plate in presence of crescent quantity of reversine. After 72 h, the plates are recovered and 100 μL ATPlite solution is added to each well. The plates are shaken for 2 min at 700 rpm and luminescence is measured using EnVision Multilabel plate reader. Each sample is analyzed in triplicate.
動物実験 動物モデル Mice bearing U14 tumors
投薬量 10 mg/kg per 3 days
投与方法 i.p.

カスタマーフィードバック

, , Mol Reprod Dev, 2013, 80(7):522-34.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Transcriptional control of pancreatic cancer immunosuppression by metabolic enzyme CD73 in a tumor-autonomous and -autocrine manner [ Nat Commun, 2023, 14(1):3364] PubMed: 37291128
The centrosomal protein 131 participates in the regulation of mitochondrial apoptosis [ Commun Biol, 2023, 6(1):1271] PubMed: 38102401
Breast cancer stem cells tolerate chromosomal instability during tumor progression via c-Jun/AXL stress signaling [ Heliyon, 2023, 9(9):e20182] PubMed: 37809421
Breast cancer stem cells tolerate chromosomal instability during tumor progression via c-Jun/AXL stress signaling [ Heliyon, 2023, 9(9):e20182] PubMed: 37809421
Transient inhibition of CDK2 activity prevents oocyte meiosis I completion and egg activation in mouse [ J Cell Physiol, 2022, 10.1002/jcp.30885] PubMed: 36161883
Integrative oncogene-dependency mapping identifies RIT1 vulnerabilities and synergies in lung cancer [ Nat Commun, 2021, 12(1):4789] PubMed: 34373451
Chemogenetic Control of Nanobodies. [ Nat Methods, 2020, 17(3):279-282] PubMed: 32066961
Acupuncture induces adenosine in fibroblasts through energy metabolism and promotes proliferation by activating MAPK signaling pathway via adenosine3 receptor. [ J Cell Physiol, 2020, 235(3):2441-2451] PubMed: 31556103
Replication stress induces mitotic death through parallel pathways regulated by WAPL and telomere deprotection. [ Nat Commun, 2019, 10(1):4224] PubMed: 31530811
Aurora-A promotes the establishment of spindle assembly checkpoint by priming the Haspin-Aurora-B feedback loop in late G2 phase [ Cell Discov, 2017, 3:16049] PubMed: 28101375

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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