Home / Cyclin-dependent Kinase Inhibitors / Ro 3306

Ro 3306

Catalog #: 4181
20 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
4181/10
4181/50
Ro 3306 | CAS No. 872573-93-8 | Cyclin-dependent Kinase Inhibitors
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Description: Cdk1 inhibitor

Chemical Name: 5-(6-Quinolinylmethylene)-2-[(2-thienylmethyl)amino]-4(5H)-thiazolone

Purity: ≥98%

Product Details
Citations (20)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

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

M.Wt:
351.45
Formula:
C18H13N3OS2
Solubility:
Soluble to 20 mM in DMSO with gentle warming
Purity:
≥98%
Storage:
Store at +4°C
CAS No:
872573-93-8

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

  1. Mitotic progression following DNA damage enables pattern recognition within micronuclei
    SM Harding, JL Benci, J Irianto, DE Discher, AJ Minn, RA Greenberg
    Nature, 2017;0(0):.
  2. CDK1 regulates mediator of DNA damage checkpoint 1 during mitotic DNA damage.
    Yu et al.
    Cancer Res., 2012;72:5448
  3. How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases?
    Jorda et al.
    J.Med.Chem., 2018;61:9105
  4. The CDK1 inhibitor RO-3306 enhances p53-mediated Bax activation and mitochondrial apoptosis in AML.
    Kojima et al.
    Cancer Sci., 2009;100:1128
  5. Selective small-molecule inhibitor reveals critical mitotic functions of human CDK1.
    Vassilev et al.
    Proc.Natl.Acad.Sci., 2006;103:10660
  6. Noninvasive monitoring of single-cell mechanics by acoustic scattering
    JH Kang, TP Miettinen, L Chen, S Olcum, G Katsikis, PS Doyle, SR Manalis
    Nat. Methods, 2019;0(0):.
  7. The Negative Cross-Talk between SAG/RBX2/ROC2 and APC/C E3 Ligases in Regulation of Cell Cycle Progression and Drug Resistance
    S Zhang, Y Shen, H Li, C Bi, Y Sun, X Xiong, W Wei, Y Sun
    Cell Rep, 2020;32(10):108102.

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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

  1. CDK4/6 inhibitors induce replication stress to cause long-term cell cycle withdrawal.
    Authors: Christos Et al.
    EMBO J  2022;41:e108599
  2. MYBL2 and ATM suppress replication stress in pluripotent stem cells.
    Authors: George Et al.
    EMBO Rep  2021;22:e51120
  3. A Biosensor for the Mitotic Kinase MPS1 Reveals Spatiotemporal Activity Dynamics and Regulation.
    Authors: Bas Et al.
    Curr Biol  2020;30:3862-3870.e6
  4. Dysfunctional telomeres trigger cellular senescence mediated by cyclic GMP-AMP synthase.
    Authors: Shibani Et al.
    J Biol Chem  2020;295:11144-11160
  5. Prolonged mitosis results in structurally aberrant and over-elongated centrioles.
    Authors: Dong Et al.
    J Cell Biol  2020;219
  6. The E3 ubiquitin ligase TRIP12 participates in cell cycle progression and chromosome stability.
    Authors: J Et al.
    Sci Rep  2020;10:789
  7. 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
  8. 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
  9. Phosphorylation of MCPH1 isoforms during mitosis followed by isoform-specific degradation by APC/C-CDH1.
    Authors: Meyer Et al.
    FASEB J  2019;33:2796
  10. PP1 and PP2A Use Opposite Phospho-dependencies to Control Distinct Processes at the Kinetochore.
    Authors: Smith Et al.
    Cell Rep  2019;28:2206
  11. 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
  12. Dynamic kinetochore size regulation promotes microtubule capture and chromosome biorientation in mitosis.
    Authors: Sacristan Et al.
    Nat Cell Biol  2018;20:800
  13. Precocious centriole disengagement and centrosome fragmentation induced by mitotic delay.
    Authors: Karki
    Nat Commun  2017;8:15803
  14. An Attachment-Independent Biochemical Timer of the Spindle Assembly Checkpoint.
    Authors: Junbin Et al.
    Mol Cell  2017;68:715-730.e5
  15. Plk1 relieves centriole block to reduplication by promoting daughter centriole maturation.
    Authors: Shukla Et al.
    Nat Commun  2015;6:8077
  16. 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
  17. 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
  18. A meta analysis of pancreatic microarray datasets yields new targets as cancer genes and biomarkers.
    Authors: Goonesekere Et al.
    PLoS One  2014;9:e93046
  19. 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
  20. 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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