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Cyclin-dependent kinase (cdk) inhibitor (reported IC50 values are 0.02 - 0.03, 0.04 - 0.2, 0.2 - 1.7 and 0.9 μM for cdk2, cdk1, cdk4 and cdk9, 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.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 241.25. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||4.15 mL||20.73 mL||41.45 mL|
|5 mM||0.83 mL||4.15 mL||8.29 mL|
|10 mM||0.41 mL||2.07 mL||4.15 mL|
|50 mM||0.08 mL||0.41 mL||0.83 mL|
References are publications that support the biological activity of the product.
Lane et al (2001) A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells. Cancer Res. 61 6170 PMID: 11507069
Yu et al (2002) SU9516, a cyclin-dependent kinase 2 inhibitor, promotes accumulation of high molecular weight E2F complexes in human colon carcinoma cells. Biochem.Pharmacol. 64 1091 PMID: 12234612
Gao et al (2006) 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 Mol.Pharmacol. 70 645 PMID: 16672643
Jorda et al (2018) How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases? J.Med.Chem 61 9105 PMID: 30234987
If you know of a relevant reference for SU 9516, please let us know.
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Keywords: SU 9516, SU 9516 supplier, Potent, cdk2, inhibitors, inhibits, Transcriptionally, downregulates, Mcl-1, proapoptotic, Cyclin-Dependent, Protein, Kinases, Bcl-2, Family, SU9516, Cyclin-dependent, Kinase, 2907, Tocris Bioscience
2 Citations for SU 9516
Citations are publications that use Tocris products. Selected citations for SU 9516 include:
Pollet et al (2018) The AHR represses nucleotide excision repair and apoptosis and contributes to UV-induced skin carcinogenesis. Cell Death Differ 25 1823 PMID: 30013037
Shi et al (2014) The FGF-1-specific single-chain antibody scFv1C9 effectively inhibits breast cancer tumour growth and metastasis. J Cell Mol Med 18 2061 PMID: 25124967
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Literature in this Area
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Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.