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Roscovitine (CYC202,Seliciclib)

InhA, Func 186692-46-6
Catalog No. ABIN3221755
  • Application
    Inhibition Assay (InhA), Functional Studies (Func)
    Purpose
    Roscovitine (Seliciclib, CYC202) is a potent and selective CDK inhibitor for Cdc2, CDK2 and CDK5 with IC50 of 0.65 μM, 0.7 μM and 0.16 μM, shows little effect on CDK4/6. Seliciclib is an orally available small molecule and cyclin-dependent kinase (CDK) inhibitor with potential apoptotic and antineoplastic activity. CDKs, serine/threonine kinases that play an important role in cell cycle regulation, are overexpressed in various malignancies. Seliciclib primarily inhibits CDK 2, 7, and 9 by competing for the ATP binding sites on these kinases, leading to a disruption of cell cycle progression. In addition, this agent seems to interfere with CDK-mediated phosphorylation of the carboxy-terminal domain of RNA polymerase II, thereby inhibiting RNA polymerase II-dependent transcription. This may lead to the down-regulation of anti-apoptotic factors, such as myeloid cell leukemia sequence 1 (Mcl-1), a protein crucial for the survival of a range of tumor cell types. The down-regulation of anti-apoptotic factors may lead to an induction of apoptosis, thereby further contributing to seliciclib's antiproliferative effects.
    Characteristics
    Target: CDK inhibitor
    Receptor: Cdc2/CDK2/CDK5
    Purification
    All the products are sent with COA, HPLC and NMR inspection report to guarantee the quality.
    Purity
    98 %
    Formula
    C19H26N6O
    Solubility
    DMSO > 100mM
  • Application Notes
    Optimal working dilution should be determined by the investigator.
    Restrictions
    For Research Use only
  • Format
    Solid
    Storage
    -20 °C
    Storage Comment
    For the majority of compounds, they could be dissolved in DMSO or other organic solvent.
    Their stock solution can be stored at -20°C for up to 3 months and aliquoted for sampling convenience.
    Several freeze/thaw cycles should not damage the activity of our small molecule products.
    However, in many instances the aqueous solutions of some compounds need to be made fresh and cannot be stored. For these compounds, their solution should be prepared just before use and stored no longer than 24 hours.
    Expiry Date
    24 months
  • Background
    Cell Cycle/Checkpoint
    Molecular Weight
    354.45 g/mol
    CAS-No
    186692-46-6
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