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Roscovitine (CYC202,Seliciclib)

InhA, Func 186692-46-6
Catalog No. ABIN3221755

Quick Overview for Roscovitine (CYC202,Seliciclib) (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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