Chemical Name: 5-(6-Quinolinylmethylene)-2-[(2-thienylmethyl)amino]-4(5H)-thiazolone
Biological ActivityATP-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).
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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.
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.
Citations for Ro 3306
The citations listed below are publications that use Tocris products. Selected citations for Ro 3306 include:
10 Citations: Showing 1 - 10
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
Phosphorylation of MCPH1 isoforms during mitosis followed by isoform-specific degradation by APC/C-CDH1.
Authors: Meyer Et al.
FASEB J 2019;33:2796
PP1 and PP2A Use Opposite Phospho-dependencies to Control Distinct Processes at the Kinetochore.
Authors: Smith Et al.
Cell Rep 2019;28:2206
Dynamic kinetochore size regulation promotes microtubule capture and chromosome biorientation in mitosis.
Authors: Sacristan Et al.
Nat Cell Biol 2018;20:800
Precocious centriole disengagement and centrosome fragmentation induced by mitotic delay.
Nat Commun 2017;8:15803
Plk1 relieves centriole block to reduplication by promoting daughter centriole maturation.
Authors: Shukla Et al.
Nat Commun 2015;6:8077
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
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
A meta analysis of pancreatic microarray datasets yields new targets as cancer genes and biomarkers.
Authors: Goonesekere Et al.
PLoS One 2014;9:e93046
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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