Reversine, an innovative inhibitor of Aurora kinases, prevents colony formation in human acute myeloid leukemia cells. It strongly inhibits Aurora kinases A and B and moderately inhibits Aurora kinase C at a concentration of 0.5 μM. In further testing, Reversine shows an IC50 of 400 nM for Aurora kinase A, 500 nM for B, and 400 nM for C, while showing limited inhibition on other tested kinases. Additionally, the IC50 for MEK1 is >1.5 μM and for muscle myosin is 350 nM[1].
体内研究
The Reversine and Aspirin combination effectively triggers cell cycle arrest and apoptosis. To assess its anti-tumor efficacy, we established a xenograft nude mouse model via subcutaneous injection. Around 16 days post-tumor inoculation, mice implanted with cervical cancer cells experienced a roughly 10% reduction in initial body weight. Nonetheless, tumor growth (tumor weight) was notably diminished, and the survival rate extended in the combination treatment group[2].
体外研究
Reversine, an innovative inhibitor of Aurora kinases, prevents colony formation in human acute myeloid leukemia cells. It strongly inhibits Aurora kinases A and B and moderately inhibits Aurora kinase C at a concentration of 0.5 μM. In further testing, Reversine shows an IC50 of 400 nM for Aurora kinase A, 500 nM for B, and 400 nM for C, while showing limited inhibition on other tested kinases. Additionally, the IC50 for MEK1 is >1.5 μM and for muscle myosin is 350 nM[1].
Reversine/逆转素 细胞实验
Cell Line
Concentration
Treated Time
Description
References
ANJEA-CD
5 µM
30 minutes
Inhibit ANJEA kinase activity
Plant Biotechnol J. 2023 Jan;21(1):63-77.
FER-CD
5 µM
30 minutes
Inhibit FER kinase activity
Plant Biotechnol J. 2023 Jan;21(1):63-77.
HERK1-CD
5 µM
30 minutes
Inhibit HERK1 kinase activity
Plant Biotechnol J. 2023 Jan;21(1):63-77.
THE1-CD
5 µM
30 minutes
Inhibit THE1 kinase activity
Plant Biotechnol J. 2023 Jan;21(1):63-77.
DDX11/C0 cells
100 nM
1 day
Reversine accelerated mitosis, reducing APC3 knockdown-induced cell death and spindle checkpoint-dependent arrest.
Nat Commun. 2015 Oct 1;6:8399.
OC2 cells
1 µM
12 hours
To evaluate the effect of Reversine on OC2 cell growth, results showed that Reversine significantly suppressed cell proliferation.
J Biomed Sci. 2012 Jan 27;19(1):9.
OCSL cells
1 µM
12 hours
To evaluate the effect of Reversine on OCSL cell growth, results showed that Reversine significantly suppressed cell proliferation.
J Biomed Sci. 2012 Jan 27;19(1):9.
Bovine ear marginal tissue fibroblasts
20 nM
2 days
Reversine-treated fibroblasts acquired the differentiation potential for neural lineage under neural-inducing (NID) conditions and expressed neural-specific markers.
Int J Biol Sci. 2016 Jan 1;12(1):53-62.
HCT116 colon cancer cells
1 µM
24 hours
To investigate the effect of Reversine on caspase-2 activity in HCT116 cells, the results showed that Reversine induced caspase-2 activation and led to the cleavage of MDM-2 protein.
Cell Death Differ. 2019 Dec;26(12):2695-2709.
C2C12 myoblasts
20 nM
4 days
Inhibits the differentiation of C2C12 myoblasts, preventing myotube formation, and increases their plasticity, allowing them to differentiate into osteoblasts and adipocytes under specific inducing conditions.
Proc Natl Acad Sci U S A. 2007 Jun 19;104(25):10482-7.
3T3E1 osteoblasts
300 nM
4 days
Increases the plasticity of 3T3E1 osteoblasts, allowing them to differentiate into adipocytes under adipocyte-inducing conditions.
Proc Natl Acad Sci U S A. 2007 Jun 19;104(25):10482-7.
Human primary skeletal myoblasts
300 nM
4 days
Increases the plasticity of human primary skeletal myoblasts, allowing them to differentiate into osteoblasts and adipocytes under specific inducing conditions.
Proc Natl Acad Sci U S A. 2007 Jun 19;104(25):10482-7.
Bovine ear marginal tissue fibroblasts
5 µM
4 days
Reversine-treated fibroblasts acquired a drastically different morphology, transformed from spindle shape into considerably larger in size, flatter, and more adhesive to the culture plate, and displayed marked cell swelling and polyploid cell formation.
Int J Biol Sci. 2016 Jan 1;12(1):53-62.
CHO cells
1000 nM
48 hours
Reversine combined with PTX significantly improved micronucleation efficiency in CHO cells and reduced cytotoxicity.
Nucleic Acids Res. 2024 Feb 9;52(3):1498-1511.
HFL1-iPS cells
1000 nM
48 hours
Reversine combined with PTX significantly improved micronucleation efficiency in HFL1-iPS cells and reduced cytotoxicity.
Nucleic Acids Res. 2024 Feb 9;52(3):1498-1511.
MCF-7 cells
5 µM
48 hours
Reversine inhibited MCF-7 cell proliferation, particularly at the tumor-stroma interface, but no additional anti-proliferative effect was observed in the bulk region.
Nat Commun. 2014 Dec 9;5:5662.
Mouse embryo cells
0.5 µM
8- to 16-cell division
Observe chromosome segregation errors, found that 48% of reversine-treated blastomeres exhibited lagging chromosomes and micronuclei formation during mitosis
Nat Commun. 2016 Mar 29;7:11165.
Mouse embryo cells
0.5 µM
four- to eighourst-cell division
Induce chromosome segregation errors, generate aneuploid cells, resulting in embryo death during peri-implantation development
Nat Commun. 2016 Mar 29;7:11165.
Mouse pre-implantation embryos
0.5 µM
four- to eighourst-cell division stage
Induced chromosome segregation errors, generating aneuploid cells and leading to embryo death during peri-implantation development.
Nat Commun. 2016 Mar 29;7:11165.
HeLa cells
0.5 µM
Inhibits MPS1 autophosphorylation, causing chromosome alignment defects, but does not affect P-S10-H3 levels
J Cell Biol. 2010 Jul 12;190(1):73-87.
HeLa cells
1 µM
Completely overrides the spindle checkpoint in the presence of 3.3 µM nocodazole, causing MAD1 and the RZZ complex to fail to localize to kinetochores
J Cell Biol. 2010 Jul 12;190(1):73-87.
Reversine/逆转素 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
NOD/SCID mice
MCF-7 breast cancer model
Intraperitoneal injection
0.5 mg/kg
Twice a week for 8 weeks
Reversine treatment inhibited MCF-7 tumor growth and bone metastasis, reducing tumor stromalization including collagen deposition and recruitment of activated stromal cells.
Nat Commun. 2014 Dec 9;5:5662.
Mice
Chromosome mosaicism model
In embryo culture medium
0.5 mM
Four- to eight-cell division stage, followed by culture in inhibitor-free medium until the mature blastocyst stage
To investigate the fate of aneuploid cells and the developmental potential of mosaic embryos, it was found that mosaic embryos have full developmental potential provided they contain sufficient euploid cells.
Nat Commun. 2016 Mar 29;7:11165.
Mice
Chromosome mosaicism model
In vitro culture
0.5 mM
Four- to eight-cell division
Investigate the fate of aneuploid cells and the developmental potential of mosaic embryos, found that reversine-treated embryos died during early postimplantation stages, but mosaic embryos containing sufficient normal euploid cells have full developmental potential
Nat Commun. 2016 Mar 29;7:11165.
SCID/Beige mice
Model of diffuse MM lesions
Intravenous injection
1 mg/kg
Twice weekly
Reversine significantly reduced tumor burden in the diffuse myeloma bone lesion model
Nat Med. 2010 Apr;16(4):483-9
Arabidopsis
Arabidopsis seedlings
Root treatment
5 μM
24 hours
Enhanced innate immunity in plant roots and thus alleviated soil-borne diseases
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