Ro 3306
Chemical Name: 5-(6-Quinolinylmethylene)-2-[(2-thienylmethyl)amino]-4(5H)-thiazolone
Purity: ≥98%
Biological Activity
Ro 3306 is an ATP-competitive cyclin-dependent kinase 1 (cdk1) inhibitor (Ki values range from 35 to 240 nM depending on cdk1 binding partner). Also reported to inhibit other cdks (Ki values are 0.89-1.32, 0.03 and >2 μM for cdk2, cdk3 and cdk4, respectively). Induces G2/M phase cell cycle arrest and apoptosis. Downregulates the expression of antiapoptotic proteins such as Bcl-2 and survivin and enhances downstream p53 signaling in acute myeloid leukemia (AML). RO 3306 also improves homology-directed repair (HDR) -mediated gene editing in hematopoietic stem and progenitor cells.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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CDK1 regulates mediator of DNA damage checkpoint 1 during mitotic DNA damage.
Yu et al.
Cancer Res., 2012;72:5448 -
How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases?
Jorda et al.
J.Med.Chem., 2018;61:9105 -
The CDK1 inhibitor RO-3306 enhances p53-mediated Bax activation and mitochondrial apoptosis in AML.
Kojima et al.
Cancer Sci., 2009;100:1128 -
Selective small-molecule inhibitor reveals critical mitotic functions of human CDK1.
Vassilev et al.
Proc.Natl.Acad.Sci., 2006;103:10660
Product Datasheets
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Citations for Ro 3306
The citations listed below are publications that use Tocris products. Selected citations for Ro 3306 include:
20 Citations: Showing 1 - 10
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CDK4/6 inhibitors induce replication stress to cause long-term cell cycle withdrawal.
Authors: Christos Et al.
EMBO J 2022;41:e108599
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MYBL2 and ATM suppress replication stress in pluripotent stem cells.
Authors: George Et al.
EMBO Rep 2021;22:e51120
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A Biosensor for the Mitotic Kinase MPS1 Reveals Spatiotemporal Activity Dynamics and Regulation.
Authors: Bas Et al.
Curr Biol 2020;30:3862-3870.e6
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Dysfunctional telomeres trigger cellular senescence mediated by cyclic GMP-AMP synthase.
Authors: Shibani Et al.
J Biol Chem 2020;295:11144-11160
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Prolonged mitosis results in structurally aberrant and over-elongated centrioles.
Authors: Dong Et al.
J Cell Biol 2020;219
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The E3 ubiquitin ligase TRIP12 participates in cell cycle progression and chromosome stability.
Authors: J Et al.
Sci Rep 2020;10:789
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Cyclin-Dependent Kinase 5 Inhibitor Butyrolactone I Elicits a Partial Agonist Activity of Peroxisome Proliferator-Activated Receptor γ.
Authors: Minsoo Et al.
Biomolecules 2020;10
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RIPK1 and Caspase-8 Ensure Chromosome Stability Independently of Their Role in Cell Death and Inflammation.
Authors: Liccardi Et al.
Mol Cell 2019;73:413
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Phosphorylation of MCPH1 isoforms during mitosis followed by isoform-specific degradation by APC/C-CDH1.
Authors: Meyer Et al.
FASEB J 2019;33:2796
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PP1 and PP2A Use Opposite Phospho-dependencies to Control Distinct Processes at the Kinetochore.
Authors: Smith Et al.
Cell Rep 2019;28:2206
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Temporal Regulation of ESCO2 Degradation by the MCM Complex, the CUL4-DDB1-VPRBP Complex, and the Anaphase-Promoting Complex.
Authors: Katsuhiko Et al.
Curr Biol 2018;28:2665-2672.e5
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Dynamic kinetochore size regulation promotes microtubule capture and chromosome biorientation in mitosis.
Authors: Sacristan Et al.
Nat Cell Biol 2018;20:800
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Precocious centriole disengagement and centrosome fragmentation induced by mitotic delay.
Authors: Karki
Nat Commun 2017;8:15803
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An Attachment-Independent Biochemical Timer of the Spindle Assembly Checkpoint.
Authors: Junbin Et al.
Mol Cell 2017;68:715-730.e5
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Plk1 relieves centriole block to reduplication by promoting daughter centriole maturation.
Authors: Shukla Et al.
Nat Commun 2015;6:8077
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JNK-associated Leucine Zipper Protein Functions as a Docking Platform for Polo-like Kinase 1 and Regulation of the Associating Transcription Factor Forkhead Box Protein K1.
Authors: Ramkumar Et al.
J Biol Chem 2015;290:29617
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A delay prior to mitotic entry triggers caspase 8-dependent cell death in p53-deficient Hela and HCT-116 cells.
Authors: Silva Et al.
Mol Cell 2015;14:1070
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A meta analysis of pancreatic microarray datasets yields new targets as cancer genes and biomarkers.
Authors: Goonesekere Et al.
PLoS One 2014;9:e93046
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Regulation of the CRL4(Cdt2) ubiquitin ligase and cell-cycle exit by the SCF(Fbxo11) ubiquitin ligase.
Authors: Rossi Et al.
Am J Physiol Gastrointest Liver Physiol 2013;49:1159
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Multi-phosphorylation of the intrinsically disordered unique domain of c-Src studied by in-cell and real-time NMR spectroscopy.
Authors: Angel R Et al.
Chembiochem 2013;14:1820-7
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