Home GPCR & G Protein Adenosine Receptor antagonist - Aurora Kinase inhibitor Reversine For research use only.

Reversine

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.

Reversine Chemical Structure

Reversine Chemical Structure

CAS No. 656820-32-5

Purity & Quality Control

Batch: S758801 DMSO]5 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.9%
99.9

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Biological Activity

Description 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.
Targets
Aurora A [3] Aurora C [3] Aurora B [3] human A3 adenosine receptor [2]
400 nM 400 nM 500 nM 0.66 μM(Ki)
In vitro
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]
Kinase Assay 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.
Cell Research Cell lines HL-60, A375, HeLa, HCT-116, T47D, and MCF-7 cell lines
Concentrations ~10 μM
Incubation Time 72 hours
Method 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.
In Vivo
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]
Animal Research Animal Models Mice bearing U14 tumors
Dosages 10 mg/kg per 3 days
Administration i.p.

Chemical Information & Solubility

Molecular Weight 393.23 Formula

C21H27N7O
CAS No. 656820-32-5 SDF Download Reversine SDF
Smiles C1CCC(CC1)NC2=NC(=NC3=C2NC=N3)NC4=CC=C(C=C4)N5CCOCC5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 5 mg/mL ( (12.71 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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