Catalog Number: 2907
Chemical Name: (Z)-1,3-Dihydro-3-(1H-imidazol-4-ylmethylene)-5-methoxy-2H-indol-2-one
Biological Activity
Potent, selective cdk2 inhibitor (IC50 values are 0.022, 0.04, 0.2, >10, >10, 18 and >100 μM for cdk2, cdk1, cdk4, PKC, p38, PDGFR and EGFR respectively). Inhibits pRb phosphorylation causing enhanced pRB/E2F complex formation and induces G1 and G2-M cell cycle arrest. Transcriptionally downregulates Mcl-1 and has antiproliferative, cytostatic and pro-apoptotic effects in vitro.
Technical Data
  • M.Wt:
    241.25
  • Formula:
    C13H11N3O2
  • Solubility:
    Soluble to 100 mM in DMSO and to 20 mM in ethanol
  • Purity:
    >99%
  • Storage:
    Store at +4°C
  • CAS No:
    377090-84-1
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells.
    Lane et al.
    Cancer Res., 2001;61:6170
  2. SU9516, a cyclin-dependent kinase 2 inhibitor, promotes accumulation of high molecular weight E2F complexes in human colon carcinoma cells.
    Yu et al.
    Biochem.Pharmacol., 2002;64:1091
  3. The three-substituted indolinone cyclin-dependent kinase 2 inhibitor 3-[1-(3H-Imidazol-4-yl)-meth-(Z)-ylidene]-5-methoxy-1,3-dihydro-indol-2-one (SU9516) kills human leukemia cells via down-regulation of Mcl-1 through a transcriptional m
    Gao et al.
    Mol.Pharmacol., 2006;70:645
Citations:

The citations listed below are publications that use Tocris products. Selected citations for SU 9516 include:

1 Citations: Showing 1 - 1

  1. The FGF-1-specific single-chain antibody scFv1C9 effectively inhibits breast cancer tumour growth and metastasis.
    Authors: Shi Et al.
    J Cell Mol Med 2014;18:2061

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