1. Cell Cycle/DNA Damage
  2. CDK

Ro-3306 

Cat. No.: HY-12529 Purity: 96.77%
Handling Instructions

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.

For research use only. We do not sell to patients.
Ro-3306 Chemical Structure

Ro-3306 Chemical Structure

CAS No. : 872573-93-8

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 92 In-stock
5 mg USD 84 In-stock
10 mg USD 119 In-stock
50 mg USD 360 In-stock
100 mg USD 624 In-stock
200 mg   Get quote  
500 mg   Get quote  

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    Ro-3306 purchased from MCE. Usage Cited in: Oncogene. 2018 Feb 27.

    HEK-293T cells are treated with the ERK1/2 inhibitor SCH772984 (0.5 µM) and/or the CDK1 inhibitor RO-3306 (9 μM) during the last 18 h of transfection. Cells are lysed after 24 h and western blot is performed with the indicated antibodies. HSP90 is used as a loading control.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    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)[1]

    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[1]. 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[2]. RO-3306 (10 μM) effectively arrests oocyte maturation. RO-3306 reduces the blastocyst formation in oocytes[3].

    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 2.8454 mL 14.2268 mL 28.4535 mL
    5 mM 0.5691 mL 2.8454 mL 5.6907 mL
    10 mM 0.2845 mL 1.4227 mL 2.8454 mL
    Please refer to the solubility information to select the appropriate solvent.
    Kinase Assay
    [1]

    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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    351.45

    Formula

    C₁₈H₁₃N₃OS₂

    CAS No.

    872573-93-8

    SMILES

    O=C1N=C(NCC2=CC=CS2)S/C1=C\C3=CC=C4N=CC=CC4=C3

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 47 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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    Product Name:
    Ro-3306
    Cat. No.:
    HY-12529
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