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Reversine Adenosine Receptor antagonist

Name: Reversine
Brand: Selleck Chemicals
SKU: S7588
Rating: 5 (16 reviews)

Cat.No.S7588

Reversine is a potent human A3 adenosine receptor antagonist with K_i 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.

Chemical Structure

Molecular Weight: 393.23

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.9

Related Targets	CXCR Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas
Other Adenosine Receptor Inhibitors	CGS 21680 HCl ZM241385 SCH58261 Etrumadenant (AB928) A2AR antagonist 1 Ciforadenant (CPI-444) Imaradenant (AZD4635) DPCPX Proxyphylline Alloxazine

Chemical Information, Storage & Stability

Molecular Weight	393.23	Formula	C₂₁H₂₇N₇O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	656820-32-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
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
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.250mg/ml (0.64mM)	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 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.250mg/ml (0.64mM)	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.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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 400 nM Aurora C 400 nM Aurora B 500 nM human A3 adenosine receptor 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. This compound, as an A3 adenosine receptor antagonist, competitively inhibits forskolin-stimulated cAMP production in stably transfected Chinese hamster ovary (CHO) cells. It inhibits the phosphorylation of a well-known Aurora target, histone H3 in HCT116 cells. Moreover, this chemical potently blocks proliferation of multiple tumour cell types, and induces cell death. In primary human tumour samples, it also inhibits colony formation of leukaemic cells. When treated in combination, this compound and aspirin synergistically inhibit growth of cervical cancer cells and induce cell apoptosis.
Kinase Assay	Radioligand Binding Assays
Kinase Assay	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 tumours, Reversine (10 mg/kg i.p.) and aspirin cause more reduced tumour weight and tumour volume when compared with the control agents.
References	[1] https://pubmed.ncbi.nlm.nih.gov/14719906/ [2] https://pubmed.ncbi.nlm.nih.gov/16033270/ [3] https://pubmed.ncbi.nlm.nih.gov/18483302/ [4] https://pubmed.ncbi.nlm.nih.gov/23475158/

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