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Submit ReviewRo 3306
Description: Cdk1 inhibitor
Chemical Name: 5-(6-Quinolinylmethylene)-2-[(2-thienylmethyl)amino]-4(5H)-thiazolone
Purity: ≥98% (HPLC)
Biological Activity for Ro 3306
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.
Compound Libraries for Ro 3306
Ro 3306 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
Technical Data for Ro 3306
| M. Wt | 351.45 |
| Formula | C18H13N3OS2 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 872573-93-8 |
| PubChem ID | 11631681 |
| InChI Key | XOLMRFUGOINFDQ-YBEGLDIGSA-N |
| Smiles | O=C2/C(SC(NCC3=CC=CS3)=N2)=C/C1=CC=C(N=CC=C4)C4=C1 |
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.
Solubility Data for Ro 3306
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 7.03 | 20 with gentle warming |
Preparing Stock Solutions for Ro 3306
The following data is based on the product molecular weight 351.45. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 14.23 mL | 71.13 mL | 142.27 mL |
| 1 mM | 2.85 mL | 14.23 mL | 28.45 mL |
| 2 mM | 1.42 mL | 7.11 mL | 14.23 mL |
| 10 mM | 0.28 mL | 1.42 mL | 2.85 mL |
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Product Datasheets for Ro 3306
References for Ro 3306
References are publications that support the biological activity of the product.
Kojima et al (2009) The CDK1 inhibitor RO-3306 enhances p53-mediated Bax activation and mitochondrial apoptosis in AML. Cancer Sci. 100 1128 PMID: 19385969
Vassilev et al (2006) Selective small-molecule inhibitor reveals critical mitotic functions of human CDK1. Proc.Natl.Acad.Sci. 103 10660 PMID: 16818887
Yu et al (2012) CDK1 regulates mediator of DNA damage checkpoint 1 during mitotic DNA damage. Cancer Res. 72 5448 PMID: 22962268
Jorda et al (2018) How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases? J.Med.Chem. 61 9105 PMID: 30234987
Azhagiri et al (2021) Homology-directed gene-editing approaches for hematopoietic stem and progenitor cell gene therapy. Stem Cell Res.Ther. 12 500 PMID: 34503562
If you know of a relevant reference for Ro 3306, please let us know.
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20 Citations for Ro 3306
Citations are publications that use Tocris products. Selected citations for Ro 3306 include:
Meyer et al (2019) Phosphorylation of MCPH1 isoforms during mitosis followed by isoform-specific degradation by APC/C-CDH1. FASEB J 33 2796 PMID: 30303738
Liccardi et al (2019) RIPK1 and Caspase-8 Ensure Chromosome Stability Independently of Their Role in Cell Death and Inflammation. Mol Cell 73 413 PMID: 30598363
Silva et al (2015) A delay prior to mitotic entry triggers caspase 8-dependent cell death in p53-deficient Hela and HCT-116 cells. Mol Cell 14 1070 PMID: 25602147
Goonesekere et al (2014) A meta analysis of pancreatic microarray datasets yields new targets as cancer genes and biomarkers. PLoS One 9 e93046 PMID: 24740004
George et al (2021) MYBL2 and ATM suppress replication stress in pluripotent stem cells. EMBO Rep 22 e51120 PMID: 33779025
Smith et al (2019) PP1 and PP2A Use Opposite Phospho-dependencies to Control Distinct Processes at the Kinetochore. Cell Rep 28 2206 PMID: 31433993
Karki (2017) Precocious centriole disengagement and centrosome fragmentation induced by mitotic delay. Nat Commun 8 15803 PMID: 28607478
Ramkumar et al (2015) 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. J Biol Chem 290 29617 PMID: 26468278
Shukla et al (2015) Plk1 relieves centriole block to reduplication by promoting daughter centriole maturation. Nat Commun 6 8077 PMID: 26293378
Rossi et al (2013) Regulation of the CRL4(Cdt2) ubiquitin ligase and cell-cycle exit by the SCF(Fbxo11) ubiquitin ligase. Am J Physiol Gastrointest Liver Physiol 49 1159 PMID: 23478441
Junbin et al (2017) An Attachment-Independent Biochemical Timer of the Spindle Assembly Checkpoint. Mol Cell 68 715-730.e5 PMID: 29129638
Katsuhiko et al (2018) Temporal Regulation of ESCO2 Degradation by the MCM Complex, the CUL4-DDB1-VPRBP Complex, and the Anaphase-Promoting Complex. Curr Biol 28 2665-2672.e5 PMID: 30100344
Angel R et al (2013) Multi-phosphorylation of the intrinsically disordered unique domain of c-Src studied by in-cell and real-time NMR spectroscopy. Chembiochem 14 1820-7 PMID: 23744817
Christos et al (2022) CDK4/6 inhibitors induce replication stress to cause long-term cell cycle withdrawal. EMBO J 41 e108599 PMID: 35037284
Sacristan et al (2018) Dynamic kinetochore size regulation promotes microtubule capture and chromosome biorientation in mitosis. Nat Cell Biol 20 800 PMID: 29915359
Minsoo et al (2020) Cyclin-Dependent Kinase 5 Inhibitor Butyrolactone I Elicits a Partial Agonist Activity of Peroxisome Proliferator-Activated Receptor γ. Biomolecules 10 PMID: 32054125
Dong et al (2020) Prolonged mitosis results in structurally aberrant and over-elongated centrioles. J Cell Biol 219 PMID: 32271878
Bas et al (2020) A Biosensor for the Mitotic Kinase MPS1 Reveals Spatiotemporal Activity Dynamics and Regulation. Curr Biol 30 3862-3870.e6 PMID: 32888483
Shibani et al (2020) Dysfunctional telomeres trigger cellular senescence mediated by cyclic GMP-AMP synthase. J Biol Chem 295 11144-11160 PMID: 32540968
J et al (2020) The E3 ubiquitin ligase TRIP12 participates in cell cycle progression and chromosome stability. Sci Rep 10 789 PMID: 31964993
Do you know of a great paper that uses Ro 3306 from Tocris? Please let us know.
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