Home GPCR & G Protein Adenosine Receptor antagonist - Aurora Kinase inhibitor Reversine

research use only

Reversine Adenosine Receptor antagonist

Cat.No.S7588

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 Adenosine Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 393.23

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 393.23 Formula

C21H27N7O

 Storage (From the date of receipt)
CAS No. 656820-32-5 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1CCC(CC1)NC2=NC(=NC3=C2NC=N3)NC4=CC=C(C=C4)N5CCOCC5

Solubility

In vitro
Batch:

DMSO : 5 mg/mL (12.71 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
Aurora A [3]
400 nM
Aurora C [3]
400 nM
Aurora B [3]
500 nM
human A3 adenosine receptor [2]
0.66 μM(Ki)
In vitro
Reversine induces myogenic lineage-committed cells to become multipotent mesenchymal progenitor cells, which proliferates and redifferentiates into bone and fat cells. [1] This compound, as an A3 adenosine receptor antagonist, competitively inhibits forskolin-stimulated cAMP production in stably transfected Chinese hamster ovary (CHO) cells. [2] It inhibits the phosphorylation of a well-known Aurora target, histone H3 in HCT116 cells. Moreover, this chemical potently blocks proliferation of multiple tumor cell types, and induces cell death. In primary human tumor samples, it also inhibits colony formation of leukemic cells. [3] When treated in combination, this compound 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.
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]
References

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.