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Reversine

Catalog No. T1825   CAS 656820-32-5

Reversine, a small synthetic purine analogue (2, 6-disubstituted purine), is a potent inhibitior of Aurora A/B/C(IC50s=150-500 nM).

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Reversine Chemical Structure
Reversine, CAS 656820-32-5
Pack Size Availability Price/USD Quantity
1 mg In stock $ 32.00
2 mg In stock $ 45.00
5 mg In stock $ 64.00
10 mg In stock $ 81.00
25 mg In stock $ 167.00
50 mg In stock $ 235.00
100 mg In stock $ 413.00
1 mL * 10 mM (in DMSO) In stock $ 64.00
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Purity: 99.75%
Purity: 98%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Reversine, a small synthetic purine analogue (2, 6-disubstituted purine), is a potent inhibitior of Aurora A/B/C(IC50s=150-500 nM).
Targets&IC50 Aurora A:150-500 nM, Aurora B:150-500 nM, Aurora C:150-500 nM
In vitro In mice carrying U14 tumors, intraperitoneal injection of Reversine (10 mg/kg) effectively reduces tumor cells.
In vivo In stably transfected Chinese hamster ovary cells, Reversine can competitively inhibit cAMP production stimulated by. In HCT116 cells, Reversine suppresses the Aurora targets and phosphorylation of histone H3. Additionally, in primary human tumor samples, Reversine is capable of inhibiting the formation of leukemia cell colonies.
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 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.(Only for Reference)
Molecular Weight 393.49
Formula C21H27N7O
CAS No. 656820-32-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 5 mg/mL (12.71 mM), Heating is recommended.

TargetMolReferences and Literature

1. Chen S, et al. J Am Chem Soc. 2004, 126(2), 410-411. 2. Perreira M, et al. J Med Chem. 2005, 48(15), 4910-4918. 3. D'Alise AM, et al. Mol Cancer Ther. 2008, 7(5), 1140-1149. 4. Qin HX, et al. Cytotechnology. 2013, 65(4), 643-653. 5. Lima K, Carlos J A E G, de Melo Alves-Paiva R, et al. Reversine exhibits antineoplastic activity in JAK2 V617F-positive myeloproliferative neoplasms[J]. Scientific reports. 2019, 9(1): 9895. 6. Carlos J A E G, Lima K, Coelho-Silva J L, et al. Reversine exerts cytotoxic effects through multiple cell death mechanisms in acute lymphoblastic leukemia[J]. Cellular Oncology. 2020: 1-11.

TargetMolCitations

1. Carlos J A E G, Lima K, Coelho-Silva J L, et al. Reversine exerts cytotoxic effects through multiple cell death mechanisms in acute lymphoblastic leukemia. Cellular Oncology. 2020: 1-11 2. Lima K, Carlos J A E G, de Melo Alves-Paiva R, et al. Reversine exhibits antineoplastic activity in JAK2 V617F-positive myeloproliferative neoplasms. Scientific Reports. 2019, 9(1): 9895 3. Tan M, Ren F, Yang X. Anti-HBV therapeutic potential of small molecule 3, 5, 6, 7, 3′, 4′-Hexamethoxyflavone in vitro and in vivo. Virology. 2021 4. Hirakata, Camila, et al. Targeting glioma cells by antineoplastic activity of reversine. Oncology Letters. 22.2 (2021): 1-9 5. Hirakata, Camila, et al. Targeting glioma cells by antineoplastic activity of reversine. Oncology Letters. 22.2 (2021): 1-9 6. Parducci N S, Garnique A D M B, Lima K, et al.Antineoplastic effects of pharmacological inhibitors of aurora kinases in CSF3RT618I-driven cells.Blood Cells, Molecules, and Diseases.2023: 102799.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Kinase Inhibitor Library Membrane Protein-targeted Compound Library Anti-Neurodegenerative Disease Compound Library GPCR Compound Library Neuronal Signaling Compound Library Target-Focused Phenotypic Screening Library Stem Cell Differentiation Compound Library Autophagy Compound Library Bioactive Compounds Library Max

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Keywords

Reversine 656820-32-5 Autophagy Cell Cycle/Checkpoint Chromatin/Epigenetic GPCR/G Protein Neuroscience Adenosine Receptor Aurora Kinase inhibit Inhibitor inhibitor

 

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