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CAS No. : 872573-93-8
|Size||Stock||Price||Quantity||Add to Cart||Quotation Online|
|Cat. No. :||CS-3790|
|CAS No. :||872573-93-8|
|M. Wt. :||351.45|
|Solubility:||DMSO: ≥ 47 mg/mL|
Ro-3306 is a potent and selective inhibitor of CDK1, with Kis of 20 nM, 35 nM and 340 nM for CDK1, CDK1/cyclin B1 and CDK2/cyclin E, respectively. IC50 & Target: Ki: 20 nM (CDK1), 35 nM (CDK1/cyclin B1), 340 nM (CDK2/cyclin E), 318 nM (PKCδ) In Vitro: RO-3306 is an ATP-competitive inhibitor, and inhibits CDK1/cyclin A complexes with Ki of 110 nM. RO-3306 blocks the cell cycle in the G2/M phase of human cancer cells. RO-3306 (4 μM) induces apoptosis in cancer cells. RO-3306 (5 μM) induces G2/M-phase cell cycle arrest and apoptosis of AML cells in a time-dependent manner. RO-3306 treatment significantly increases the percentage of Annexin V-positive cells in G1-phase cells without affecting the cell cycle distribution. RO-3306 enhances p53-mediated apoptosis. RO-3306 cooperates with Nutlin-3 in activating Bax and inducing mitochondrial apoptosis. RO-3306 (5 μM) downregulates antiapoptotic p21, Bcl-2 and survivin protein expression in AML. RO-3306 inhibits p53-induced p21 synthesis. RO-3306 does not inhibit RNA polymerase II CTD phosphorylation. RO-3306 (10 μM) effectively arrests oocyte maturation. RO-3306 reduces the blastocyst formation in oocytes.
Protocol:Kinase Assay: The CDK assays are run by using recombinant human CDK/cyclin complexes (CDK1/cyclin B1, CDK1/cyclin A, CDK2/cyclin E, and CDK4/cyclin D) expressed and isolated from Hi5 insect cells. GST-cyclin B1, CDK1, GST-cyclin-E, CDK2, GST-CDK4, and cyclin D, are used in the assay. The GST-tagged proteins are coexpressed and purified in complex with their partners. All assays use a His-6-tagged fragment of pRB (amino acids 385-928) as a substrate. The protein is expressed from a construct. It is expressed in M15 Escherichia coli cells and bound on a Ni-chalated agarose column pretreated with 1 mM imidazole and eluted with 500 mM imidazole. The eluted protein is dialyzed against 20 mM Hepes, pH 7/6.25 mM MgCl2/1.5 mM DTT, aliquoted, and stored at −80°C.
Jang WI, et al. A specific inhibitor of CDK1, RO-3306, reversibly arrests meiosis during in vitro maturation of porcine oocytes. Anim Reprod Sci. 2014 Jan 30;144(3-4):102-8.
Vassilev LT, et al. Selective small-molecule inhibitor reveals critical mitotic functions of human CDK1. Proc Natl Acad Sci U S A. 2006 Jul 11;103(28):10660-5.
Kojima K, et al. Cyclin-dependent kinase 1 inhibitor RO-3306 enhances p53-mediated Bax activation and mitochondrial apoptosis in AML. Cancer Sci. 2009 Jun;100(6):1128-36.
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