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Reversine

Cat. No. M2188
Reversine Structure
Size Price Availability Quantity
5mg USD 78  USD78 In stock
10mg USD 100  USD100 In stock
25mg USD 190  USD190 In stock
50mg USD 280  USD280 In stock
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Quality Control & Documentation
Biological Activity

Reversine is a novel class of ATP-competitive Aurora kinase inhibitors. Reversine inhibits the phosphorylation of histone H3, a direct downstream target of Aurora kinases. Similarly to the Aurora kinase inhibitor VX-680, reversine inhibited colony formation of leukemic cells from patients with acute myeloid leukemia but was significantly less toxic than VX-680 on cells from healthy donors. Reversine can increase the plasticity of C2C12 myoblasts at the single-cell level and that reversine-treated cells gain the ability to differentiate into osteoblasts and adipocytes under lineage-specific inducing conditions. Moreover, reversine is active in multiple cell types, including 3T3E1 osteoblasts and human primary skeletal myoblasts. Cultured myoblasts treated for four days with 5 μM reversine were dedifferentiated into confluent stem cell progenitors, that could then be induced by osteogenic or adipogenic medium to re-differentiate into bone or adipose precursors, respectively.

Chemical Information
Molecular Weight 393.49
Formula C21H27N7O
CAS Number 656820-32-5
Solubility (25°C) DMSO 10 mM
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] D'Alise AM, et al. Mol Cancer Ther. Reversine, a novel Aurora kinases inhibitor, inhibits colony formation of human acute myeloid leukemia cells.

[2] Chen S, et al. Proc Natl Acad Sci U S A. Reversine increases the plasticity of lineage-committed mammalian cells.

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Keywords: Reversine supplier, Aurora Kinase, inhibitors, activators


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